Ritonavir (Synonyms: 利托那韋; ABT 538; RTV)

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Ritonavir (ABT 538) 是用于研究 HIV 感染和 AIDS 的 HIV 蛋白酶的抑制劑。Ritonavir 也是 SARS-CoV 3CL^pro 的抑制劑，IC₅₀ 為 1.61 μM。

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Ritonavir Chemical Structure

CAS No. : 155213-67-5

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規(guī)格	價格	是否有貨
10 mM * 1 mL in DMSO	￥517	In-stock
5 mg	￥293	In-stock
10 mg	￥470	In-stock
50 mg	￥1100	In-stock
100 mg	￥1850	In-stock
500 mg	￥4663	In-stock
1 g		詢價
5 g		詢價

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MCE 顧客使用本產(chǎn)品發(fā)表的 24 篇科研文獻

•Cancer Cell. 2024 Nov 11;42(11):1955-1969.e7. [Abstract]
•Signal Transduct Target Ther. 2021 May 29;6(1):212. [Abstract]
•Nat Commun. 2020 Sep 4;11(1):4417. [Abstract]
•Antivir Res. 2020 Jun;178:104786. [Abstract]
•Int J Antimicrob Agents. 2019 Dec;54(6):814-819. [Abstract]
•Environ Pollut. 2024 May 25:124214. [Abstract]
•Surfaces and Interfaces. 2023 Aug, 40, 103096.
•Aging Cell. 2022 Dec 20;e13750. [Abstract]
•J Agric Food Chem. 2022 Feb 21. [Abstract]
•Biomed Pharmacother. 2020 Sep;129:110506. [Abstract]
•Antiviral Res. 2022 Nov 10;105463. [Abstract]
•Antimicrob Agents Chemother. 2020 Aug 20;64(9):e00872-20. [Abstract]

•Vet Sci. 2023 Aug 9, 10(8), 513.
•J Hum Genet. 2020 Jan;65(2):143-153. [Abstract]
•Drug Metab Dispos. 2019 Sep;47(9):954-960. [Abstract]
•J Liq ChromaTogr R T. 2019: 1-9.
•Res Sq. 2024 Nov 21.
•SSRN. 2024 Jan 26.
•Curr Protoc. 2021 Feb;1(2):e32. [Abstract]
•Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Transmissores de Hematozoários. 2020 Sep.
•bioRxiv. 2020 Apr.
•Faculty of Pharmacy in Hradec Králové Department of Pharmacological and Toxicology. University of Oxford. 2019 Jul.
•Department of Analytical Chemistry. Charles University. 2019 Jun.
•Chem Cent J. 2017 Jan 3;11:1. [Abstract]

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生物活性
純度 & 產(chǎn)品資料
參考文獻

生物活性

Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 1.61 μM.

細胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CCRF-CEM	EC₅₀	115 nM Compound: RTV	Antiviral activity against HIV2 ROD with protease V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay Antiviral activity against HIV2 ROD with protease V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay	[PMID: 17576848]
CCRF-CEM	EC₅₀	310 nM Compound: RTV	Antiviral activity against HIV2 ROD with protease G17N mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay Antiviral activity against HIV2 ROD with protease G17N mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay	[PMID: 17576848]
CCRF-CEM	EC₅₀	421 nM Compound: RTV	Antiviral activity against wild type HIV2 ROD infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay Antiviral activity against wild type HIV2 ROD infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay	[PMID: 17576848]
CCRF-CEM	EC₅₀	84 nM Compound: RTV	Antiviral activity against HIV2 ROD with protease G17N/V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay Antiviral activity against HIV2 ROD with protease G17N/V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay	[PMID: 17576848]
HEK293	IC₅₀	> 300 μM Compound: ritonavir	Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	0.08 μM Compound: ritonavir	Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis	[PMID: 23241029]
HEK293	IC₅₀	0.7 μM Compound: Ritonavir	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate	[PMID: 22587986]
HEK293	IC₅₀	1 μM Compound: Ritonavir	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate	[PMID: 22587986]
HEK293	IC₅₀	1.3 μM Compound: Ritonavir	Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting	[PMID: 22541068]
HEK293	IC₅₀	1.7 μM Compound: Ritonavir	Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method	[PMID: 21030469]
HEK293	IC₅₀	23.7 μM Compound: ritonavir	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	24.8 μM Compound: ritonavir	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	3 μM Compound: Ritonavir	Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method	[PMID: 21030469]
HEK293	IC₅₀	33.9 μM Compound: ritonavir	Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	4.4 μM Compound: ritonavir	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	4.4 μM Compound: ritonavir	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	4.4 μM Compound: Ritonavir	Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting	[PMID: 22541068]
HEK293	IC₅₀	5 μM Compound: Ritonavir	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate	[PMID: 22587986]
HEK293	IC₅₀	6.1 μM Compound: Ritonavir	Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting	[PMID: 22541068]
Hepatocyte	IC₅₀	34.2 nM Compound: Ritonavir	Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs	[PMID: 18212104]
HepG2	CC₅₀	18.4 μM Compound: RTV	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 5 days by XTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 5 days by XTT assay	10.1039/C1MD00147G
HepG2	EC₅₀	4 μM Compound: Ritonavir	Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis	[PMID: 20966043]
HuT78	CC₅₀	> 145 μM Compound: Ritonavir	Cytotoxicity against human HUT78 cells assessed as reduction in cell viability after 5 days by MTT assay Cytotoxicity against human HUT78 cells assessed as reduction in cell viability after 5 days by MTT assay	[PMID: 26613134]
HuT78	EC₅₀	29 μM Compound: Ritonavir	Antiviral activity against HIV1 3B persistently infected in HUT78 cells assessed as reduction of p24 production after 43 hrs by ELISA Antiviral activity against HIV1 3B persistently infected in HUT78 cells assessed as reduction of p24 production after 43 hrs by ELISA	[PMID: 26613134]
LLC-PK1	IC₅₀	> 50 μM Compound: Ritonavir	Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	> 50 μM Compound: Ritonavir	Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	12 μM Compound: Ritonavir	Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
MDCK-II	IC₅₀	2.1 μM Compound: ritonavir	Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis	[PMID: 23241029]
MT2	EC₅₀	0.038 μM Compound: RTV	Antiviral activity against HIV1 LAI infected in human MT2 cells after 7 days by MTT assay Antiviral activity against HIV1 LAI infected in human MT2 cells after 7 days by MTT assay	[PMID: 18955518]
MT2	EC₅₀	0.054 μM Compound: ritonavir, RTV	Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT2	EC₅₀	0.21 μM Compound: ritonavir, RTV	Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT2	EC₅₀	0.26 μM Compound: ritonavir, RTV	Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT2	CC₅₀	21.3 μM Compound: RTV	Cytotoxicity against human MT2 cells by MTT assay Cytotoxicity against human MT2 cells by MTT assay	[PMID: 18955518]
MT2	CC₅₀	31.1 μM Compound: ritonavir, RTV	Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT2	EC₅₀	32.2 nM Compound: RTV	Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as virus-induced cytopathic effect after 5 days by XTT assay Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as virus-induced cytopathic effect after 5 days by XTT assay	10.1039/C1MD00147G
MT2	CC₅₀	65 μM Compound: RTV	Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay	10.1039/C1MD00147G
MT4	EC₅₀	> 1 μM Compound: RTV	Antiviral activity against HIV1 NL4-3 harboring L10I/G48V/I54V/L90M amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of saquinavir by ELISA Antiviral activity against HIV1 NL4-3 harboring L10I/G48V/I54V/L90M amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of saquinavir by ELISA	[PMID: 18955518]
MT4	EC₅₀	> 1 μM Compound: RTV	Antiviral activity against HIV1 NL4-3 harboring L10F/V32I/M46I/I54M//A71V/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of amprenavir by ELISA Antiviral activity against HIV1 NL4-3 harboring L10F/V32I/M46I/I54M//A71V/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of amprenavir by ELISA	[PMID: 18955518]
MT4	EC₅₀	> 1 μM Compound: RTV	Antiviral activity against HIV1 NL4-3 harboring L10F/L24I/M46I/L63P/A71V/G73S/V82T amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of indinavir by ELISA Antiviral activity against HIV1 NL4-3 harboring L10F/L24I/M46I/L63P/A71V/G73S/V82T amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of indinavir by ELISA	[PMID: 18955518]
MT4	EC₅₀	> 1 μM Compound: RTV	Antiviral activity against HIV1 NL4-3 harboring M46I/V82F/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of ritonavir by ELISA Antiviral activity against HIV1 NL4-3 harboring M46I/V82F/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of ritonavir by ELISA	[PMID: 18955518]
MT4	EC₅₀	> 1 μM Compound: RTV	Antiviral activity against HIV1 NL4-3 harboring L10F/M46I/I54V/V82A amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of Lopinavir by ELISA Antiviral activity against HIV1 NL4-3 harboring L10F/M46I/I54V/V82A amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of Lopinavir by ELISA	[PMID: 18955518]
MT4	CC₅₀	> 1 μM Compound: Ritonavir	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay	[PMID: 29934245]
MT4	EC₅₀	> 1 μM Compound: ritonavir, RTV	Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	> 1 μM Compound: ritonavir, RTV	Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	> 1 μM Compound: ritonavir, RTV	Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	> 1 μM Compound: ritonavir, RTV	Antiviral activity against lopinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against lopinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	CC₅₀	> 5.55 μM Compound: Ritonavir	Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay	[PMID: 26613134]
MT4	EC₅₀	0.0015 μM Compound: Ritonavir	Antiviral activity against wild type HIV1 3B infected in human MT4 LTR-EGFP cells by EGFP reporter gene assay Antiviral activity against wild type HIV1 3B infected in human MT4 LTR-EGFP cells by EGFP reporter gene assay	[PMID: 22765892]
MT4	EC₅₀	0.021 μM Compound: RTV	Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of p24 gag protein production by ELISA Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of p24 gag protein production by ELISA	[PMID: 18955518]
MT4	EC₅₀	0.022 μM Compound: ABT-538	Anti-HIV activity against MT-4 cells using a cytopathicity assay Anti-HIV activity against MT-4 cells using a cytopathicity assay	10.1016/0960-894X(95)00462-3
MT4	EC₅₀	0.033 μM Compound: ritonavir, RTV	Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.039 μM Compound: ritonavir	Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.041 μM Compound: ritonavir	Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.042 μM Compound: ritonavir	Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.043 μM Compound: ritonavir	Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18378713]
MT4	ED₅₀	0.05 μg/mL Compound: 2	In vitro anti-HIV activity in MT-4 cells by using an HIV cytopathic assay In vitro anti-HIV activity in MT-4 cells by using an HIV cytopathic assay	[PMID: 9748353]
MT4	EC₅₀	0.051 μM Compound: ritonavir, RTV	Antiviral activity against nelfinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against nelfinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.055 μM Compound: ritonavir	Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18378713]
MT4	EC₅₀	0.058 μM Compound: ritonavir	Antiviral activity against HIV 1 NL4.3 integrase E92Q mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV 1 NL4.3 integrase E92Q mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18378713]
MT4	EC₅₀	0.06 μM Compound: ritonavir	Antiviral activity against HIV 1 NL4.3 harboring integrase L74M mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV 1 NL4.3 harboring integrase L74M mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18378713]
MT4	EC₅₀	0.06 μM Compound: ritonavir	Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.061 μM Compound: RTV	Antiviral activity against wild type HIV1 NL4-3 infected in MT4 cells after 6 days by MTT assay Antiviral activity against wild type HIV1 NL4-3 infected in MT4 cells after 6 days by MTT assay	[PMID: 17638694]
MT4	EC₅₀	0.069 μM Compound: ritonavir	Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.069 μM Compound: ritonavir	Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.07 μM Compound: Ritonavir	Anti-HIV activity was determined in MT-4 cells in the presence of 0% human serum using cytopathic effect assay Anti-HIV activity was determined in MT-4 cells in the presence of 0% human serum using cytopathic effect assay	[PMID: 9934466]
MT4	EC₅₀	0.08 μM Compound: RTV	Antiviral activity against HIV1 NL4-3 harboring L10F/D30N/K45I/A71V/T74S amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of nelfinavir by ELISA Antiviral activity against HIV1 NL4-3 harboring L10F/D30N/K45I/A71V/T74S amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of nelfinavir by ELISA	[PMID: 18955518]
MT4	EC₅₀	0.09 μM Compound: Ritonavir	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 26613134]
MT4	EC₅₀	0.09 μM Compound: ritonavir	Antiviral activity against HIV 1 NL4.3 integrase S230N mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV 1 NL4.3 integrase S230N mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18378713]
MT4	EC₅₀	0.12 μM Compound: ritonavir, RTV	Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.13 μM Compound: ritonavir, RTV	Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.14 μM Compound: RTV	Antiviral activity against HIV1 NL4-3 harboring L23I/K43I/M46I/I50L/G51A/A71V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of atazanavir by ELISA Antiviral activity against HIV1 NL4-3 harboring L23I/K43I/M46I/I50L/G51A/A71V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of atazanavir by ELISA	[PMID: 18955518]
MT4	EC₅₀	0.14 μM Compound: Ritonavir	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 26613134]
MT4	EC₅₀	0.26 μM Compound: RTV	Antiviral activity against HIV1 NL4-3 harboring L10F/L33F/M46I/I47V/Q58E/V82I/I84V/I85V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of GRL-02031 by E Antiviral activity against HIV1 NL4-3 harboring L10F/L33F/M46I/I47V/Q58E/V82I/I84V/I85V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of GRL-02031 by E	[PMID: 18955518]
MT4	EC₅₀	0.29 μM Compound: ritonavir, RTV	Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.3 μM Compound: ritonavir, RTV	Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.38 μM Compound: ritonavir, RTV	Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.81 μM Compound: Ritonavir	Anti-HIV activity was determined in MT-4 cells in the presence of 50% human serum using cytopathic effect assay Anti-HIV activity was determined in MT-4 cells in the presence of 50% human serum using cytopathic effect assay	[PMID: 9934466]
MT4	CC₅₀	17000 nM Compound: Ritonavir, RTV	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 18426195]
MT4	CC₅₀	26 μM Compound: RTV	Cytotoxicity against human MT4 cells after 6 days by MTT assay Cytotoxicity against human MT4 cells after 6 days by MTT assay	[PMID: 17638694]
MT4	EC₅₀	349 nM Compound: RTV	Antiviral activity against HIV2 MS infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV2 MS infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 17576848]
MT4	EC₅₀	36 nM Compound: Ritonavir, RTV	Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of viral-induced cytopathic effect by MTT method Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of viral-induced cytopathic effect by MTT method	[PMID: 18426195]
MT4	EC₅₀	36 nM Compound: Ritonavir	Antiviral activity against HIV1 3B in MT4 cells by MTT assay Antiviral activity against HIV1 3B in MT4 cells by MTT assay	[PMID: 17537628]
MT4	EC₅₀	46 nM Compound: RTV	Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 17576848]
MT4	EC₅₀	50 nM Compound: RTV	Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 6 days by XTT assay Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 6 days by XTT assay	[PMID: 19961222]

體外研究
(In Vitro)

Ritonavir (ABT 538) 是 CYP3A4 介導(dǎo)的睪酮 6β-羥基化抑制劑，平均 K_i 為 19 nM，也抑制甲苯磺丁脲羥基化，IC₅₀ 為 4.2 μM^[1]。
Ritonavir (ABT 538) 被發(fā)現(xiàn)是 CYP3A 介導(dǎo)的生物轉(zhuǎn)化的有效抑制劑 (nifedipine oxidation with IC₅₀ of 0.07 mM，17alpha-ethynylestradiol 2-hydroxylation with IC₅₀ 2 mM；terfenadine hydroxylation，IC₅₀ 為 0.14 mM)。Ritonavir 還是 CYP2D6 (IC₅₀=2.5 mM) 和 CYP2C9/10 (IC₅₀=8.0 mM) 介導(dǎo)的反應(yīng)的抑制劑^[2]。
Ritonavir 導(dǎo)致未感染的人 PBMC 培養(yǎng)物中的細胞活力增加。Ritonavir 顯著降低 PBMC 對細胞凋亡的易感性，與較低水平的 caspase-1 表達相關(guān)，減少膜聯(lián)蛋白 V 染色，并降低未感染的人 PBMC 培養(yǎng)物中的 caspase-3 活性。Ritonavir 在無毒濃度下以時間和劑量依賴性方式抑制 PBMC 和單核細胞誘導(dǎo)腫瘤壞死因子 (TNF) 的產(chǎn)生^[3]。
Ritonavir 抑制 p-糖蛋白介導(dǎo)的沙奎那韋擠壓作用，IC₅₀ 為 0.2 μM，表明 Ritonavir 對 p-糖蛋白具有高親和力^[4]。
Ritonavir 有效抑制 ABT-378 的人肝微粒體代謝，K_i 為 13 nM。Ritonavir 與 ABT-378 聯(lián)合使用 (比例為 3:1 和 29:1) 抑制 CYP3A (IC₅₀=1.1 和 4.6 μM)，盡管不如 Ritonavir (IC₅₀=0.14 μM)^[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

720.94

Formula

C₃₇H₄₈N₆O₅S₂

CAS 號

155213-67-5

性狀

固體

顏色

White to off-white

中文名稱

利托那韋；瑞托納韋

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性數(shù)據(jù)

細胞實驗：

DMSO 中的溶解度 : 25 mg/mL (34.68 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	1.3871 mL	6.9354 mL	13.8708 mL
5 mM	0.2774 mL	1.3871 mL	2.7742 mL
10 mM	0.1387 mL	0.6935 mL	1.3871 mL

查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

摩爾計算器
稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動物實驗：

請根據(jù)您的實驗動物和給藥方式選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

方案一

請依序添加每種溶劑： 0.5% CMC-Na/1% Tween-80 in Saline water
Solubility: 10 mg/mL (13.87 mM); 懸濁液; 超聲助溶
方案二

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (3.47 mM); 懸濁液; 超聲助溶

此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案三

請依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: 2.5 mg/mL (3.47 mM); 澄清溶液; 加熱助溶

此方案可獲得 2.5 mg/mL的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

方案一

請依序添加每種溶劑： 17% Solutol HS-15 in Saline
Solubility: 10 mg/mL (13.87 mM); 懸濁液; 超聲助溶

動物溶解方案計算器

請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

每只動物的給藥體積

μL

動物數(shù)量

只

由于實驗過程有損耗，建議您多配一只動物的量

請輸入您的動物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購。，Tween 80，均可在 MCE 網(wǎng)站選購。

計算結(jié)果

工作液所需濃度 : mg/mL

儲備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。

動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。

請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.96%

選擇批次：

Data Sheet (644 KB) SDS (393 KB)

COA (286 KB) HNMR (282 KB) RP-HPLC (250 KB) LCMS (94 KB) OR (170 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻

[1]. Eagling VA, et al. Differential inhibition of cytochrome P450 isoforms by the protease inhibitors, ritonavir, saquinavir and indinavir. Br J Clin Pharmacol. 1997 Aug;44(2):190-4. [Content Brief]

[2]. Kumar GN, et al. Cytochrome P450-mediated metabolism of the HIV-1 protease inhibitor ritonavir (ABT-538) in human liver microsomes. J Pharmacol Exp Ther. 1996 Apr;277(1):423-31. [Content Brief]

[3]. Weichold FF, et al. HIV-1 protease inhibitor ritonavir modulates susceptibility to apoptosis of uninfected T cells. J Hum Virol. 1999 Sep-Oct;2(5):261-9. [Content Brief]

[4]. Drewe J, et al. HIV protease inhibitor ritonavir: a more potent inhibitor of P-glycoprotein than the cyclosporine analog SDZ PSC 833. Biochem Pharmacol. 1999 May 15;57(10):1147-52. [Content Brief]

[5]. Kumar GN, et al. Potent inhibition of the cytochrome P-450 3A-mediated human liver microsomal metabolism of a novel HIV protease inhibitor by ritonavir: A positive drug-drug interaction. Drug Metab Dispos. 1999 Aug;27(8):902-8. [Content Brief]

[6]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. [Content Brief]

Ritonavir 相關(guān)分類

完整儲備液配制表

可選溶劑	濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.3871 mL	6.9354 mL	13.8708 mL	34.6769 mL
	5 mM	0.2774 mL	1.3871 mL	2.7742 mL	6.9354 mL
	10 mM	0.1387 mL	0.6935 mL	1.3871 mL	3.4677 mL
	15 mM	0.0925 mL	0.4624 mL	0.9247 mL	2.3118 mL
	20 mM	0.0694 mL	0.3468 mL	0.6935 mL	1.7338 mL
	25 mM	0.0555 mL	0.2774 mL	0.5548 mL	1.3871 mL
	30 mM	0.0462 mL	0.2312 mL	0.4624 mL	1.1559 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ritonavir155213-67-5ABT 538 RTV利托那韋瑞托納韋ABT538ABT-538HIV ProteaseHIVSARS-CoVApoptosisHuman immunodeficiency virusSARS coronavirusInhibitorinhibitorinhibit

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Ritonavir (Synonyms: 利托那韋; ABT 538; RTV)

Customer Review

Other Forms of Ritonavir:

MCE 顧客使用本產(chǎn)品發(fā)表的 24 篇科研文獻

Ritonavir 相關(guān)產(chǎn)品

•相關(guān)化合物庫:

•同靶點產(chǎn)品:

•同靶點蛋白產(chǎn)品:

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生物活性

純度 & 產(chǎn)品資料

參考文獻

摩爾計算器

稀釋計算器

Ritonavir 相關(guān)分類

完整儲備液配制表

Keywords:

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Ritonavir (Synonyms: 利托那韋; ABT 538; RTV)

Customer Review

Other Forms of Ritonavir:

Ritonavir 相關(guān)抗體

MCE 顧客使用本產(chǎn)品發(fā)表的 24 篇科研文獻

Ritonavir 相關(guān)產(chǎn)品

•相關(guān)化合物庫:

•同靶點產(chǎn)品:

•同靶點蛋白產(chǎn)品:

查看 HIV 亞型特異性產(chǎn)品:

生物活性

純度 & 產(chǎn)品資料

參考文獻

Ritonavir 相關(guān)抗體:

摩爾計算器

稀釋計算器

Ritonavir 相關(guān)分類

完整儲備液配制表

Keywords:

您最近查看的產(chǎn)品:

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