Rilpivirine (Synonyms: 利匹韋林; R278474; TMC278; DB08864)

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Rilpivirine (R278474) 是一種有效和特異性的二芳基嘧啶 (DAPY) 非核苷逆轉(zhuǎn)錄酶抑制劑 (NNRTI)。Rilpivirine 對野生型 HIV (EC₅₀=0.4 nM) 和突變體 (EC₅₀=0.1-2.0 nM) 具有很高的抗病毒活性。Rilpivirine 對 HIV 耐藥性的形成產(chǎn)生了高度的遺傳障礙。

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Rilpivirine Chemical Structure

CAS No. : 500287-72-9

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10 mM * 1 mL in DMSO	￥1100	In-stock
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Other Forms of Rilpivirine:

MCE 顧客使用本產(chǎn)品發(fā)表的 9 篇科研文獻(xiàn)

•Int J Antimicrob Agents. 2019 Dec;54(6):814-819. [Abstract]
•Br J Cancer. 2023 Jan 30. [Abstract]
•Pharmaceuticals. 2022, 15(10), 1186.
•Sci Rep. 2015 Oct 29;5:15806. [Abstract]
•PLoS One. 2021 Mar 10;16(3):e0248139. [Abstract]
•Biol Pharm Bull. 2016;39(3):450-4. [Abstract]
•SSRN. 2023 Sep 8.
•University of Rijeka. Derartment of biotechnology
•Faculty of Pharmacy in Hradec Králové Department of Pharmacological and Toxicology. University of Oxford. 2019 Jul.

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HIV HIV-1 HIV-2

生物活性
純度 & 產(chǎn)品資料
參考文獻(xiàn)

生物活性

Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC₅₀=0.4 nM) and mutant viruses (EC₅₀=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV^[1]^[2].

IC₅₀ & Target

HIV-1

細(xì)胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.5 μM Compound: 2; RPV	Inhibition of human ERG expressed in HEK293 cells by whole cell electrophysiology assay Inhibition of human ERG expressed in HEK293 cells by whole cell electrophysiology assay	[PMID: 32293182]
HOS	CC₅₀	10 μM Compound: Rilpivirine	Cytotoxicity against human HOS cells assessed as reduction in cell viability measured after 48 hrs Cytotoxicity against human HOS cells assessed as reduction in cell viability measured after 48 hrs	[PMID: 35175760]
MT2	CC₅₀	> 1 μM Compound: 39, Rilpivirine, R278474	Cytotoxicity against human MT2 cells infected with HIV1 NL4.3 by MTT assay Cytotoxicity against human MT2 cells infected with HIV1 NL4.3 by MTT assay	[PMID: 22081993]
MT2	EC₅₀	0.00065 μM Compound: rpv, 2, rilpivirine, R278474	Antiviral activity against wild type HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay Antiviral activity against wild type HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay	[PMID: 25408842]
MT2	EC₅₀	0.00065 μM Compound: Rilpivirine	Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay	[PMID: 23937980]
MT2	EC₅₀	0.00065 μM Compound: Rilpivirine	Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method	[PMID: 23298809]
MT2	EC₅₀	0.00067 μM Compound: rpv, 2, rilpivirine, R278474	Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay	[PMID: 25408842]
MT2	EC₅₀	0.00067 μM Compound: Rilpivirine	Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay	[PMID: 23937980]
MT2	EC₅₀	0.00067 μM Compound: Rilpivirine	Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method	[PMID: 23298809]
MT2	EC₅₀	0.001 μM Compound: Rilpivirine	Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathogenicity by MTT assay Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathogenicity by MTT assay	[PMID: 23899617]
MT2	EC₅₀	0.002 μM Compound: rpv, 2, rilpivirine, R278474	Antiviral activity against wild type HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay Antiviral activity against wild type HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay	[PMID: 25408842]
MT2	EC₅₀	0.002 μM Compound: Rilpivirine	Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay	[PMID: 23937980]
MT2	EC₅₀	0.002 μM Compound: Rilpivirine	Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase K103N and Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase K103N and Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method	[PMID: 23298809]
MT2	EC₅₀	0.49 nM Compound: 1b	Antiviral activity against HIV1 3B infected in human MT2 cells measured on day 4 post infection by p24 ELISA method Antiviral activity against HIV1 3B infected in human MT2 cells measured on day 4 post infection by p24 ELISA method	[PMID: 27070547]
MT2	CC₅₀	8 μM Compound: Rilpivirine	Cytotoxicity against human MT2 cells assessed as cell growth inhibition after 5 days by MTT assay Cytotoxicity against human MT2 cells assessed as cell growth inhibition after 5 days by MTT assay	[PMID: 33603971]
MT2	EC₅₀	8 μM Compound: Rilpivirine	Cytotoxicity against human MT2 cells assessed as cell viability by MTT assay Cytotoxicity against human MT2 cells assessed as cell viability by MTT assay	[PMID: 35175760]
MT2	CC₅₀	8 μM Compound: Rilpivirine	Cytotoxicity against human MT2 cells infected with wild-type HIV1 NL4-3 measured 48 hrs by MTT assay Cytotoxicity against human MT2 cells infected with wild-type HIV1 NL4-3 measured 48 hrs by MTT assay	[PMID: 31281023]
MT2	CC₅₀	8 μM Compound: Rilpivirine	Cytotoxicity against human MT2 cells assessed as growth inhibition by MTT method Cytotoxicity against human MT2 cells assessed as growth inhibition by MTT method	[PMID: 27485603]
MT2	CC₅₀	8 μM Compound: rpv, 2, rilpivirine, R278474	Cytotoxicity against human MT2 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human MT2 cells assessed as reduction in cell viability by MTT assay	[PMID: 25408842]
MT2	CC₅₀	8 μM Compound: Rilpivirine	Cytotoxicity against human MT2 cells by MTT assay Cytotoxicity against human MT2 cells by MTT assay	[PMID: 23899617]
MT2	EC₅₀	9.03 nM Compound: 1b	Antiviral activity against multi-NRTI resistant HIV1 A17 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells measured on day 4 post infection by p24 ELISA method Antiviral activity against multi-NRTI resistant HIV1 A17 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells measured on day 4 post infection by p24 ELISA method	[PMID: 27070547]
MT4	CC₅₀	> 4 μM Compound: 2	Cytotoxicity against in human MT-4 cells after 5 days by MTT assay Cytotoxicity against in human MT-4 cells after 5 days by MTT assay	[PMID: 33851529]
MT4	CC₅₀	> 4 μM Compound: RPV; 2	Cytotoxicity against mock infected human MT4 cells by MTT assay Cytotoxicity against mock infected human MT4 cells by MTT assay	[PMID: 34197708]
MT4	EC₅₀	0.0004 μM Compound: TMC278	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 23707918]
MT4	EC₅₀	0.00052 μM Compound: TMC-278	Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 V370A mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 V370A mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA	[PMID: 22818973]
MT4	EC₅₀	0.00055 μM Compound: TMC-278	Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA	[PMID: 22818973]
MT4	EC₅₀	0.001 μM Compound: TMC278	Antiviral activity against HIV1 RES056 expressing RT K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 RES056 expressing RT K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 23707918]
MT4	EC₅₀	0.1 nM Compound: 1, TMC278	Antiviral activity against HIV1 LAI with RT K103N mutation in MT4 cells by EGFP based replication assay Antiviral activity against HIV1 LAI with RT K103N mutation in MT4 cells by EGFP based replication assay	[PMID: 17223230]
MT4	EC₅₀	0.5 nM Compound: TMC278	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	[PMID: 23137340]
MT4	EC₅₀	0.5 nM Compound: TMC278	Antiviral activity against HIV1 expressing wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay Antiviral activity against HIV1 expressing wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	[PMID: 23137340]
MT4	EC₅₀	0.5 nM Compound: 1, TMC278	Antiviral activity against HIV1 LAI with RT L100I mutation in MT4 cells by EGFP based replication assay Antiviral activity against HIV1 LAI with RT L100I mutation in MT4 cells by EGFP based replication assay	[PMID: 17223230]
MT4	EC₅₀	0.5 nM Compound: 1, TMC278	Antiviral activity against HIV1 LAI with RT F227C mutation in MT4 cells by EGFP based replication assay Antiviral activity against HIV1 LAI with RT F227C mutation in MT4 cells by EGFP based replication assay	[PMID: 17223230]
MT4	EC₅₀	0.5 nM Compound: 1, TMC278	Antiviral activity against HIV1 LAI with RT F227C and V106A mutation in MT4 cells by EGFP based replication assay Antiviral activity against HIV1 LAI with RT F227C and V106A mutation in MT4 cells by EGFP based replication assay	[PMID: 17223230]
MT4	EC₅₀	1 nM Compound: 1, TMC278	Antiviral activity against wild type HIV1 LAI infected in MT4 cells by EGFP based replication assay Antiviral activity against wild type HIV1 LAI infected in MT4 cells by EGFP based replication assay	[PMID: 17223230]
MT4	EC₅₀	1.2 nM Compound: 1, TMC278	Antiviral activity against HIV1 LAI with RT Y188L mutation in MT4 cells by EGFP based replication assay Antiviral activity against HIV1 LAI with RT Y188L mutation in MT4 cells by EGFP based replication assay	[PMID: 17223230]
MT4	EC₅₀	1.3 nM Compound: TMC278	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	[PMID: 23137340]
MT4	EC₅₀	1.3 nM Compound: 1, TMC278	Antiviral activity against HIV1 LAI with RT Y181C mutation in MT4 cells by EGFP based replication assay Antiviral activity against HIV1 LAI with RT Y181C mutation in MT4 cells by EGFP based replication assay	[PMID: 17223230]
MT4	CC₅₀	2000 nM Compound: 1, TMC278	Cytotoxicity against human MT4 cells after 3 days by EGFP based replication assay Cytotoxicity against human MT4 cells after 3 days by EGFP based replication assay	[PMID: 17223230]
MT4	EC₅₀	3.2 nM Compound: 1, TMC278	Antiviral activity against HIV1 LAI with RT K103N and Y181C mutation in MT4 cells by EGFP based replication assay Antiviral activity against HIV1 LAI with RT K103N and Y181C mutation in MT4 cells by EGFP based replication assay	[PMID: 17223230]
MT4	EC₅₀	3.7 nM Compound: TMC278	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	[PMID: 23137340]
MT4	CC₅₀	3.98 μM Compound: RPV	Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay	[PMID: 36411036]
MT4	CC₅₀	3.98 μM Compound: RPV	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay	[PMID: 35061384]
MT4	CC₅₀	3.98 μM Compound: RPV	Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay	[PMID: 34496571]
MT4	CC₅₀	3.98 μM Compound: RPV	Cytotoxicity in mock-infected human MT4 assessed as reduction in cell viability incubated for 5 days by MTT assay Cytotoxicity in mock-infected human MT4 assessed as reduction in cell viability incubated for 5 days by MTT assay	[PMID: 33734714]
MT4	CC₅₀	3.98 μM Compound: 2; RPV	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay	[PMID: 32293182]
MT4	CC₅₀	3.98 μM Compound: RPV	Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay	[PMID: 34432448]
MT4	CC₅₀	4.38 μM Compound: RPV, TMC278; 2	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: 30721060]
MT4	EC₅₀	7.5 nM Compound: 1, TMC278	Antiviral activity against HIV1 LAI with RT L100I and K103N mutation in MT4 cells by EGFP based replication assay Antiviral activity against HIV1 LAI with RT L100I and K103N mutation in MT4 cells by EGFP based replication assay	[PMID: 17223230]
MT4	CC₅₀	8 μM Compound: 39, Rilpivirine, R278474	Cytotoxicity against human MT4 cells infected with HIV1 NL4.3 by MTT assay Cytotoxicity against human MT4 cells infected with HIV1 NL4.3 by MTT assay	[PMID: 22081993]
PBMC	EC₅₀	0.07 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG035 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG035 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.07 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype E isolate 93TH073 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype E isolate 93TH073 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.07 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92RW020 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92RW020 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.08 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype E isolate 92TH006 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype E isolate 92TH006 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.08 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype B isolate WEJO infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype B isolate WEJO infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.11 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 93MW959 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 93MW959 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.16 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR020 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR020 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.19 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR029 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR029 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.23 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype B isolate 93BR021 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype B isolate 93BR021 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.24 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92UG037 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92UG037 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.25 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype G isolate G3 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype G isolate G3 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.26 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG001 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG001 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.26 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype G isolate JV1083 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype G isolate JV1083 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.33 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 92BR025 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 92BR025 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.38 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG024 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG024 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.44 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92UG029 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92UG029 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.51 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype G isolate RU132 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype G isolate RU132 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.51 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype B isolate JR-CSF infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype B isolate JR-CSF infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.53 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 93IN101 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 93IN101 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	0.95 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR019 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR019 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	1.01 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype E isolate CMU08 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype E isolate CMU08 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	2.88 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype O isolate BCF02 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype O isolate BCF02 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	3.13 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype O misolate BCF01 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype O misolate BCF01 infected in human PBMC cells by cell based assay	[PMID: 19933797]
PBMC	EC₅₀	8.45 nM Compound: TMC278, rilpivirine	Antiviral activity against Human immunodeficiency virus 1 subtype O isolate BCF03 infected in human PBMC cells by cell based assay Antiviral activity against Human immunodeficiency virus 1 subtype O isolate BCF03 infected in human PBMC cells by cell based assay	[PMID: 19933797]
T-cell	EC₅₀	1142 nM Compound: Rilpivirine	Antiviral activity against HIV-1 X4 expressing reverse transcriptase K101P mutant infected in human CD4+ T cells for 3 days by FACS analysis Antiviral activity against HIV-1 X4 expressing reverse transcriptase K101P mutant infected in human CD4+ T cells for 3 days by FACS analysis	[PMID: 26487915]
T-cell	EC₅₀	13 nM Compound: Rilpivirine	Antiviral activity against HIV-1 X4 expressing wild-type reverse transcriptase infected in human CD4+ T cells for 3 days by FACS analysis Antiviral activity against HIV-1 X4 expressing wild-type reverse transcriptase infected in human CD4+ T cells for 3 days by FACS analysis	[PMID: 26487915]
T-cell	EC₅₀	13 nM Compound: Rilpivirine	Antiviral activity against HIV-1 X4 expressing reverse transcriptase K103N mutant infected in human CD4+ T cells for 3 days by FACS analysis Antiviral activity against HIV-1 X4 expressing reverse transcriptase K103N mutant infected in human CD4+ T cells for 3 days by FACS analysis	[PMID: 26487915]
T-cell	EC₅₀	51 nM Compound: Rilpivirine	Antiviral activity against HIV-1 X4 expressing reverse transcriptase Y181C mutant infected in human CD4+ T cells for 3 days by FACS analysis Antiviral activity against HIV-1 X4 expressing reverse transcriptase Y181C mutant infected in human CD4+ T cells for 3 days by FACS analysis	[PMID: 26487915]
TZM	CC₅₀	> 30 μM Compound: 1b	Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability after 1 day by CytoTox-Glo assay Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability after 1 day by CytoTox-Glo assay	[PMID: 27070547]
TZM	CC₅₀	> 341 nM Compound: RPV; TMC278	Cytotoxicity against human TZM-bl cells by CytoTox-Glo reagent-based assay Cytotoxicity against human TZM-bl cells by CytoTox-Glo reagent-based assay	[PMID: 29635166]
TZM	CC₅₀	19.4 μM Compound: 2	Cytotoxicity against human TZM-bl cells after 4 days by XTT assay Cytotoxicity against human TZM-bl cells after 4 days by XTT assay	[PMID: 22856541]

體外研究
(In Vitro)

R278474 is active against wild-type HIV-1 (EC₅₀=0.4 nM) and all single and double mutants tested (EC₅₀=0.1-2.0 nM)^[1].
R278474 (10-5000 nM; 30 d) does not observe the sign of wild-type HIV-1 breakthrough at 1 μM within 30 days^[1].
R278474 inhibits 81% of clinical isolates (about 1200 recombinant clinical isolates) at a 50% inhibitory concentration (EC₅₀) less than 1 nM, and inhibits 94% at EC₅₀ less than 10 nM^[1].
TMC278 shows subnanomolar EC₅₀s against wild-type HIV-1 group M isolates (0.07-1.01 nM) and nanomolar EC₅₀s against group O isolates (2.88-8.45 nM) in MT4 T-cells^[2].

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

體內(nèi)研究
(In Vivo)

R278474 (10-160 mg/kg; p.o. for 1 month) does not produce abnormal effects in rat, apart from liver weight increase and species-specific thyroid hypertrophy, both at the higher dose levels^[1].
R278474 (i.v.) exhibits elimination half-life ranges from 4.4 h in rat to 31 h in dog, and exposure (AUC_inf) amounts to 3.1 μg?h/mL (4 mg/kg) in rat, 8.7 μg?h/mL (1.25 mg/kg) in dog, 1.4 μg?h/mL (1.25 mg/ kg) in monkey, and 44?μg h/mL (1.25 mg/kg) in rabbit^[1].
R278474 (p.o.) exhibits half-life ranges between 2.8 h in rat and 39 h in dog, and oral bioavailability of 32% and 31% in rat and dog^[1].

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

Clinical Trial

分子量

366.42

Formula

C₂₂H₁₈N₆

CAS 號

500287-72-9

性狀

固體

顏色

Light yellow to yellow

中文名稱

利匹韋林；利吡韋林

運(yùn)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	1 year
	-20°C	6 months

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : 50 mg/mL (136.46 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	2.7291 mL	13.6455 mL	27.2911 mL
5 mM	0.5458 mL	2.7291 mL	5.4582 mL
10 mM	0.2729 mL	1.3646 mL	2.7291 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, 1 year; -20°C, 6 months。-80°C儲存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?jiān)?個月內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)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(shí)驗(yàn)：

請根據(jù)您的實(shí)驗(yàn)動物和給藥方式選擇適當(dāng)?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(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (8.19 mM); 澄清溶液

此方案可獲得 ≥ 3 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 30.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 3 mg/mL (8.19 mM); 懸濁液; 超聲助溶

此方案可獲得 3 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 30.0 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: ≥ 3 mg/mL (8.19 mM); 澄清溶液

此方案可獲得 ≥ 3 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個月以上的動物實(shí)驗(yàn)酌情使用。
以 1 mL 工作液為例，取 100 μL 30.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

動物溶解方案計(jì)算器

請輸入動物實(shí)驗(yàn)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(shí)驗(yàn)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(jì)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(shí)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(shí)驗(yàn)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(jǐn)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: 99.71%

選擇批次：

Data Sheet (628 KB) SDS (392 KB)

COA (188 KB) LCMS (268 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[1]. Janssen PAJ, et, al. In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine). J Med Chem. 2005 Mar 24;48(6):1901-9. [Content Brief]

[2]. Azijn H, et, al. TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. Antimicrob Agents Chemother. 2010 Feb;54(2):718-27. [Content Brief]

Rilpivirine 相關(guān)分類

Infection

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	2.7291 mL	13.6455 mL	27.2911 mL	68.2277 mL
	5 mM	0.5458 mL	2.7291 mL	5.4582 mL	13.6455 mL
	10 mM	0.2729 mL	1.3646 mL	2.7291 mL	6.8228 mL
	15 mM	0.1819 mL	0.9097 mL	1.8194 mL	4.5485 mL
	20 mM	0.1365 mL	0.6823 mL	1.3646 mL	3.4114 mL
	25 mM	0.1092 mL	0.5458 mL	1.0916 mL	2.7291 mL
	30 mM	0.0910 mL	0.4549 mL	0.9097 mL	2.2743 mL
	40 mM	0.0682 mL	0.3411 mL	0.6823 mL	1.7057 mL
	50 mM	0.0546 mL	0.2729 mL	0.5458 mL	1.3646 mL
	60 mM	0.0455 mL	0.2274 mL	0.4549 mL	1.1371 mL
	80 mM	0.0341 mL	0.1706 mL	0.3411 mL	0.8528 mL
	100 mM	0.0273 mL	0.1365 mL	0.2729 mL	0.6823 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.

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Rilpivirine (Synonyms: 利匹韋林; R278474; TMC278; DB08864)

Customer Review

Other Forms of Rilpivirine:

MCE 顧客使用本產(chǎn)品發(fā)表的 9 篇科研文獻(xiàn)

Rilpivirine 相關(guān)產(chǎn)品

•相關(guān)化合物庫:

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)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(xiàn)

摩爾計(jì)算器

稀釋計(jì)算器

Rilpivirine 相關(guān)分類

完整儲備液配制表

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Rilpivirine (Synonyms: 利匹韋林; R278474; TMC278; DB08864)

Customer Review

Other Forms of Rilpivirine:

Rilpivirine 相關(guān)抗體

MCE 顧客使用本產(chǎn)品發(fā)表的 9 篇科研文獻(xiàn)

Rilpivirine 相關(guān)產(chǎn)品

•相關(guān)化合物庫:

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)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(xiàn)

Rilpivirine 相關(guān)抗體:

摩爾計(jì)算器

稀釋計(jì)算器

Rilpivirine 相關(guān)分類

完整儲備液配制表

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