Tipranavir (Synonyms: 替拉那韋; PNU-140690)

目錄號(hào): HY-15148 純度: ≥98.0%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南技術(shù)支持

Tipranavir (PNU-140690) 有效抑制 HIV-1 蛋白酶酶活性和二聚化，對(duì)抗多種蛋白酶抑制劑(PI)的HIV-1分離株具有有效的活性，IC₅₀ 為 66-410 nM。Tipranavir 抑制 SARS-CoV-2 3CL^pro 活性。

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Tipranavir Chemical Structure

CAS No. : 174484-41-4

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可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3. 試用裝只面向終端客戶(hù)。

規(guī)格	價(jià)格	是否有貨
10 mM * 1 mL in DMSO	￥4375	In-stock
1 mg	￥950	In-stock
5 mg	￥3300	In-stock
10 mg	￥4950	In-stock
50 mg		詢(xún)價(jià)
100 mg		詢(xún)價(jià)

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Customer Review

Other Forms of Tipranavir:

Tipranavir-d₄ 詢(xún)價(jià)
Tipranavir-d₇ 詢(xún)價(jià)
Tipranavir (Standard) 詢(xún)價(jià)

MCE 顧客使用本產(chǎn)品發(fā)表的 10 篇科研文獻(xiàn)

•Signal Transduct Target Ther. 2021 May 29;6(1):212. [Abstract]
•Sci Adv. 2023 Jul 14;9(28):eadg2955. [Abstract]
•Nat Commun. 2020 Sep 4;11(1):4417. [Abstract]
•Int J Antimicrob Agents. 2019 Dec;54(6):814-819. [Abstract]
•Talanta. 2018 May 1;181:182-189. [Abstract]
•Antimicrob Agents Chemother. 2020 Aug 20;64(9):e00872-20. [Abstract]
•ACS Chem Biol. 2014 Jul 18;9(7):1622-31. [Abstract]
•Research Square Print. 2022 May.
•bioRxiv. 2020 Apr.
•Faculty of Pharmacy in Hradec Králové Department of Pharmacological and Toxicology. University of Oxford. 2019 Jul.

Tipranavir 相關(guān)產(chǎn)品

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HIV HIV-1 HIV-2

生物活性
實(shí)驗(yàn)參考方法
純度 & 產(chǎn)品資料
參考文獻(xiàn)

生物活性

Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC₅₀s of 66-410 nM^[1]^[2]. Tipranavir inhibits SARS-CoV-2 3CL^pro activity^[3].

IC₅₀ & Target

HIV-1

細(xì)胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
H9	IC₅₀	0.03 μM Compound: 39b	Inhibition of HIV-1 protease in a cell culture assay using HIV-1 IIIB infected H9 cells. Inhibition of HIV-1 protease in a cell culture assay using HIV-1 IIIB infected H9 cells.	[PMID: 9719600]
MT2	EC₅₀	0.17 μM Compound: TPV	Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay	[PMID: 20439612]
MT2	EC₅₀	0.3 μM Compound: TPV	Antiviral activity against HIV2 EHO infected in human MT2 cells by MTT assay Antiviral activity against HIV2 EHO infected in human MT2 cells by MTT assay	[PMID: 20439612]
MT2	EC₅₀	0.33 μM Compound: TPV	Antiviral activity against HIV2 ROD infected in human MT2 cells by MTT assay Antiviral activity against HIV2 ROD infected in human MT2 cells by MTT assay	[PMID: 20439612]
MT2	CC₅₀	54.1 μM Compound: TPV	Cytotoxicity against human MT2 cells after 7 days by MTT assay Cytotoxicity against human MT2 cells after 7 days by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.022 μM Compound: TPV	Antiviral activity against HIV1 expressing protease L10I/G48V/I54V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of saquinavir by MTT assay Antiviral activity against HIV1 expressing protease L10I/G48V/I54V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of saquinavir by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.029 μM Compound: TPV	Antiviral activity against HIV1 expressing protease L10I/L24I/M46I/V82I/I84V mutant infected in human MT4 cells selected after 50 passages of GRL-216 by MTT assay Antiviral activity against HIV1 expressing protease L10I/L24I/M46I/V82I/I84V mutant infected in human MT4 cells selected after 50 passages of GRL-216 by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.037 μM Compound: TPV	Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.039 μM Compound: TPV	Antiviral activity against HIV1 expressing protease L10F/D30N/K45I/A71V/T74S mutant infected in human MT4 cells selected at 5 uM of nelfinavir by MTT assay Antiviral activity against HIV1 expressing protease L10F/D30N/K45I/A71V/T74S mutant infected in human MT4 cells selected at 5 uM of nelfinavir by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.042 μM Compound: TPV	Antiviral activity against HIV1 expressing protease L10F/M46M,I/Q61Q mutant infected in human MT4 cells selected at 1 uM of GRL-396 by MTT assay Antiviral activity against HIV1 expressing protease L10F/M46M,I/Q61Q mutant infected in human MT4 cells selected at 1 uM of GRL-396 by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.095 μM Compound: TPV	Antiviral activity against HIV1 expressing protease L10F/M46I/T91S mutant infected in human MT4 cells selected at 1 uM of GRL-246 by MTT assay Antiviral activity against HIV1 expressing protease L10F/M46I/T91S mutant infected in human MT4 cells selected at 1 uM of GRL-246 by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.22 μM Compound: TPV	Antiviral activity against HIV1 expressing protease L10F/M46I/I50V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of amprenavir by MTT assay Antiviral activity against HIV1 expressing protease L10F/M46I/I50V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of amprenavir by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.31 μM Compound: TPV	Antiviral activity against HIV1 expressing protease L10F/M46I/I54V/V82A mutant infected in human MT4 cells selected at 5 uM of Lopinavir by MTT assay Antiviral activity against HIV1 expressing protease L10F/M46I/I54V/V82A mutant infected in human MT4 cells selected at 5 uM of Lopinavir by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.32 μM Compound: TPV	Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.41 μM Compound: TPV	Antiviral activity against HIV1 expressing protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells selected at 5 uM of atazanavir by MTT assay Antiviral activity against HIV1 expressing protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells selected at 5 uM of atazanavir by MTT assay	[PMID: 20439612]
MT4	EC₅₀	184 nM Compound: TPV	Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in absence of human serum by MTT assay Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in absence of human serum by MTT assay	[PMID: 18212102]
MT4	EC₅₀	204 nM Compound: TPV	Antiviral activity against wild-type HIV1 RF infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in absence of human serum by MTT assay Antiviral activity against wild-type HIV1 RF infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in absence of human serum by MTT assay	[PMID: 18212102]
MT4	EC₅₀	310 nM Compound: TPV	Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 10% human serum by MTS assay Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 10% human serum by MTS assay	[PMID: 17620375]
MT4	EC₅₀	360 nM Compound: TPV	Antiviral activity against HIV1 A17 infected in human MT4 cells harboring protease L10F, V32I, M46I, I47V, Q58E, and I84V mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infection meas Antiviral activity against HIV1 A17 infected in human MT4 cells harboring protease L10F, V32I, M46I, I47V, Q58E, and I84V mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infection meas	[PMID: 18212102]
MT4	EC₅₀	40.9 nM Compound: TPV	Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum by MTS assay Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum by MTS assay	[PMID: 17620375]
MT4	EC₅₀	507 nM Compound: TPV	Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 20% human serum by MTS assay Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 20% human serum by MTS assay	[PMID: 17620375]
MT4	EC₅₀	580 nM Compound: TPV	Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 30% human serum by MTS assay Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 30% human serum by MTS assay	[PMID: 17620375]
MT4	EC₅₀	66 nM Compound: TPV	Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity after 5 days post dose by MTT assay Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity after 5 days post dose by MTT assay	[PMID: 18212102]
MT4	EC₅₀	660 nM Compound: TPV	Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 40% human serum by MTS assay Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 40% human serum by MTS assay	[PMID: 17620375]
MT4	EC₅₀	7839 nM Compound: TPV	Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in presence of 50% human serum by MTT assay Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in presence of 50% human serum by MTT assay	[PMID: 18212102]
PBMC	EC₅₀	0.12 μM Compound: TPV	Antiviral activity against wild type HIV1 ERS104 containing protease L36P mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against wild type HIV1 ERS104 containing protease L36P mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.18 μM Compound: TPV	Antiviral activity against multidrug-resistant HIV1 isolate B containing protease L10I, K14R, L33I, M36I,M46I, F53I, K55R, I62V, L63P, A71V, G73S, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate B containing protease L10I, K14R, L33I, M36I,M46I, F53I, K55R, I62V, L63P, A71V, G73S, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.23 μM Compound: TPV	Antiviral activity against multidrug-resistant HIV1 isolate JSL containing L10I, L24I, I33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, and V82A mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate JSL containing L10I, L24I, I33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, and V82A mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.24 μM Compound: TPV	Antiviral activity against multidrug-resistant HIV1 isolate G containing L10I, V11I, T12E, I15V, L19I,R41K, M46L, L63P, A71T, V82A, and L90M mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate G containing L10I, V11I, T12E, I15V, L19I,R41K, M46L, L63P, A71T, V82A, and L90M mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.35 μM Compound: TPV	Antiviral activity against multidrug-resistant HIV1 isolate MM containing L10I, K43T, M46L, I54V, L63P, A71V, V82A, L90M, and Q92K mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate MM containing L10I, K43T, M46L, I54V, L63P, A71V, V82A, L90M, and Q92K mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.38 μM Compound: TPV	Antiviral activity against multidrug-resistant HIV1 isolate C containing protease L10I, I15V, K20R, L24I, M36I, M46L, I54V, I62V, L63P, K70Q, V82A, and L89M mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate C containing protease L10I, I15V, K20R, L24I, M36I, M46L, I54V, I62V, L63P, K70Q, V82A, and L89M mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.38 μM Compound: TPV	Antiviral activity against multidrug-resistant HIV1 isolate TM containing L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate TM containing L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]

體外研究
(In Vitro)

Tipranavir (PNU-140690) 抑制HIV-1蛋白酶的酶活性，阻止蛋白酶亞基的二聚化，并對(duì)廣泛譜系的野生型和多重蛋白酶抑制劑（PI）耐藥的HIV-1變異株表現(xiàn)出強(qiáng)大的活性。當(dāng)包含HIV_B和HIV_C在內(nèi)的11種多重PI耐藥（但對(duì)Tipranavir敏感）的臨床分離株混合物（HIV_11MIX）被用于篩選對(duì)Tipranavir的耐藥性時(shí)，HIV_11MIX迅速（在10輪傳代 [HIV_11MIX^P10] 后）獲得了高水平的Tipranavir (PNU-140690) 耐藥性，并能在高濃度的Tipranavir (PNU-140690) 下復(fù)制。cHIV_B^I54V 和 cHIV_B^I54V/V82T 對(duì)Tipranavir (PNU-140690) 顯示出顯著的耐藥性，其IC₅₀ 分別為2.9 μM 和 3.2 μM，這比針對(duì)cHIV_B 的IC₅₀ 分別增加了11倍和12倍^[1]。

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

體內(nèi)研究
(In Vivo)

Tipranavir (PNU-140690) 每天口服兩次，必須與低劑量利托那韋 (RTV) 聯(lián)合使用以提高 Tipranavir 的生物利用度。在 Tipranavir/r 聯(lián)合處理的小鼠中，肝臟、脾臟和眼睛中的 Tipranavir (PNU-140690) 豐度顯著高于僅用 Tipranavir 處理的小鼠。替拉那韋 (PNU-140690) 代謝物在單獨(dú)替拉那韋組的血清和肝臟中占 31% 和 38%。在 Tipranavir (PNU-140690) 和 Tipranavir (TPV/r) 聯(lián)合處理的小鼠中，在血清和肝臟中僅檢測(cè)到 1% 和 2% 的代謝物。Sprague-Dawley 大鼠單次服用[¹⁴C]Tipranavir (PNU-140690)，同時(shí)服用 RTV。糞便中最豐富的代謝物是氧化代謝物。在尿液中，沒(méi)有發(fā)現(xiàn)明顯存在的單一代謝物^[2]。

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

Clinical Trial

分子量

602.66

Formula

C₃₁H₃₃F₃N₂O₅S

CAS 號(hào)

174484-41-4

性狀

固體

顏色

White to off-white

中文名稱(chēng)

替拉那韋

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : 200 mg/mL (331.86 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

Ethanol 中的溶解度 : ≥ 50 mg/mL (82.97 mM)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	1.6593 mL	8.2966 mL	16.5931 mL
5 mM	0.3319 mL	1.6593 mL	3.3186 mL
10 mM	0.1659 mL	0.8297 mL	1.6593 mL

查看完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(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(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)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(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 5 mg/mL (8.30 mM); 懸濁液; 超聲助溶

此方案可獲得 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 50.0 mg/mL 的澄清 DMSO 儲(chǔ)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(qǐng)依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (8.30 mM); 澄清溶液

此方案可獲得 ≥ 5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。
以 1 mL 工作液為例，取 100 μL 50.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。
方案三

請(qǐng)依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.15 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 EtOH 儲(chǔ)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。
方案四

請(qǐng)依序添加每種溶劑： 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.15 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 EtOH 儲(chǔ)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。
方案五

請(qǐng)依序添加每種溶劑： 10% EtOH 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.15 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 EtOH 儲(chǔ)備液加到 900 μL 玉米油中，混合均勻。
方案六

請(qǐng)依序添加每種溶劑： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 2.5 mg/mL (4.15 mM); 懸濁液; 超聲助溶

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)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(guò) 2%。

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

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)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(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)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: ≥98.0%

選擇批次：

Data Sheet (652 KB) SDS (393 KB)

COA (286 KB) HNMR (271 KB) MS (68 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[1]. Aoki M, et al. Loss of the protease dimerization inhibition activity of tipranavir (TPV) and its association with the acquisition of resistance to TPV by HIV-1. J Virol. 2012 Dec;86(24):13384-96. [Content Brief]

[2]. Li F, et al. Metabolism-mediated drug interactions associated with ritonavir-boosted tipranavir in mice. Drug Metab Dispos. 2010 May;38(5):871-8. [Content Brief]

[3]. 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]

Animal Administration ^[2]	Mice^[2] All mice (2-4 months old) are maintained under a standard 12-h dark and 12-h light cycle with water and chow provided ad libitum. For metabolomic analysis, Tipranavir (PNU-140690) (40 mg/kg) is administered via ball-tipped gavage needles, and the mice are housed in separate metabolic cages for 18 h. Urine and feces samples are collected and stored at ?20°C for further analysis. For tissue distribution and inhibition studies, three groups of mice are used and are orally treated with Tipranavir (100 mg/kg), RTV (40 mg/kg), and Tipranavir (PNU-140690) (100 mg/kg Tipranavir and 40 mg/kg RTV), respectively. Tissues including the liver, brain, lung, kidney, spleen, and eyes are collected 30 min after treatment and stored at ?20°C for further analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)	[1]. Aoki M, et al. Loss of the protease dimerization inhibition activity of tipranavir (TPV) and its association with the acquisition of resistance to TPV by HIV-1. J Virol. 2012 Dec;86(24):13384-96. [Content Brief] [2]. Li F, et al. Metabolism-mediated drug interactions associated with ritonavir-boosted tipranavir in mice. Drug Metab Dispos. 2010 May;38(5):871-8. [Content Brief] [3]. 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]

Animal Administration
^[2]

Mice^[2]
All mice (2-4 months old) are maintained under a standard 12-h dark and 12-h light cycle with water and chow provided ad libitum. For metabolomic analysis, Tipranavir (PNU-140690) (40 mg/kg) is administered via ball-tipped gavage needles, and the mice are housed in separate metabolic cages for 18 h. Urine and feces samples are collected and stored at ?20°C for further analysis. For tissue distribution and inhibition studies, three groups of mice are used and are orally treated with Tipranavir (100 mg/kg), RTV (40 mg/kg), and Tipranavir (PNU-140690) (100 mg/kg Tipranavir and 40 mg/kg RTV), respectively. Tissues including the liver, brain, lung, kidney, spleen, and eyes are collected 30 min after treatment and stored at ?20°C for further analysis.

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

參考文獻(xiàn)

[1]. Aoki M, et al. Loss of the protease dimerization inhibition activity of tipranavir (TPV) and its association with the acquisition of resistance to TPV by HIV-1. J Virol. 2012 Dec;86(24):13384-96. [Content Brief]

[2]. Li F, et al. Metabolism-mediated drug interactions associated with ritonavir-boosted tipranavir in mice. Drug Metab Dispos. 2010 May;38(5):871-8. [Content Brief]

[3]. 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]

Tipranavir 相關(guān)分類(lèi)

Infection

完整儲(chǔ)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

Ethanol / DMSO	1 mM	1.6593 mL	8.2966 mL	16.5931 mL	41.4828 mL
	5 mM	0.3319 mL	1.6593 mL	3.3186 mL	8.2966 mL
	10 mM	0.1659 mL	0.8297 mL	1.6593 mL	4.1483 mL
	15 mM	0.1106 mL	0.5531 mL	1.1062 mL	2.7655 mL
	20 mM	0.0830 mL	0.4148 mL	0.8297 mL	2.0741 mL
	25 mM	0.0664 mL	0.3319 mL	0.6637 mL	1.6593 mL
	30 mM	0.0553 mL	0.2766 mL	0.5531 mL	1.3828 mL
	40 mM	0.0415 mL	0.2074 mL	0.4148 mL	1.0371 mL
	50 mM	0.0332 mL	0.1659 mL	0.3319 mL	0.8297 mL
	60 mM	0.0277 mL	0.1383 mL	0.2766 mL	0.6914 mL
	80 mM	0.0207 mL	0.1037 mL	0.2074 mL	0.5185 mL
DMSO	100 mM	0.0166 mL	0.0830 mL	0.1659 mL	0.4148 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:

Tipranavir174484-41-4PNU-140690替拉那韋PNU140690PNU 140690HIV ProteaseHIVSARS-CoVHuman immunodeficiency virusSARS coronavirusInhibitorinhibitorinhibit

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Tipranavir (Synonyms: 替拉那韋; PNU-140690)

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生物活性

實(shí)驗(yàn)參考方法

純度 & 產(chǎn)品資料

參考文獻(xiàn)

摩爾計(jì)算器

稀釋計(jì)算器

Tipranavir 相關(guān)分類(lèi)

完整儲(chǔ)備液配制表

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Tipranavir (Synonyms: 替拉那韋; PNU-140690)

Customer Review

Other Forms of Tipranavir:

Tipranavir 相關(guān)抗體

MCE 顧客使用本產(chǎn)品發(fā)表的 10 篇科研文獻(xiàn)

Tipranavir 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

•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

實(shí)驗(yàn)參考方法

純度 & 產(chǎn)品資料

參考文獻(xiàn)

Tipranavir 相關(guān)抗體:

摩爾計(jì)算器

稀釋計(jì)算器

Tipranavir 相關(guān)分類(lèi)

完整儲(chǔ)備液配制表

Keywords:

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