安瑞那韋作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetAmprenavirCat. No.: HY-17430CAS No.: 161814-49-9分式: CHNOS分量: 505.63作靶點(diǎn): HIV; HIV Protease作通路: Anti-infection; Metabolic Enzyme/Protease儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (197.77 mM)* means soluble, but saturation unknown

2、.SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 1.9777 mL 9.8887 mL 19.7773 mL5 mM 0.3955 mL 1.9777 mL 3.9555 mL10 mM 0.1978 mL 0.9889 mL 1.9777 mL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；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)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適

3、當(dāng)?shù)娜芙獍?。以下溶解案都?qǐng)先按照 In Vitro 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 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)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；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/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.94 mM); Clear solution此案可獲得 2.5 mg/mL (4.94 mM，飽和度未知) 的澄清溶液。以 1

4、 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.94 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (4.94 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的

5、澄 DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.94 mM); Clear solution此案可獲得 2.5 mg/mL (4.94 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Amprenavir (VX-478)HIV蛋酶抑制劑，Ki為0.6 n

6、M。IC & Target IC50 Value: 0.6 nM (Ki); Against wild-type clinical HIV isolates:14.6 +/- 12.5 ng/mL (mean +/- SD) 1.Target: HIVprotease體外研究 Amprenavir has an enzyme inhibition constant (Ki = 0.6 nM) that falls within the Ki range of the other proteaseinhibitors. Amprenavirs in vitro 50% inhibitory co

7、ncentration (IC50) against wild-type clinical HIV isolates is 14.6 +/-12.5 ng/mL (mean +/- SD) 1. Amprenavir had direct inhibitory effects on invasion of Huh-7 hepatocarcinoma celllines, inhibiting MMP proteolytic activation 2.體內(nèi)研究 Amprenavir was able to promote regression of hepatocarcinoma growth

8、in vivo by anti-angiogenetic and overall anti- tumor activities, independently by PI3K/AKT related pathways that at today is one of the more suggestive hypothesis to explain the anti-tumor effects of the different protease inhibitors 2. Amprenavir efficiently activated PXR andinduced PXR target gene

9、 expression in vitro and in vivo. Short-term exposure to amprenavirsignificantly increasedplasma total cholesterol and atherogenic low-density lipoprotein cholesterol levels in wild-type mice, but not in PXR-deficient mice 3. Amprenavir has been approved for adults and children; the recommended caps

10、ule doses are 1200mg twice daily for adults and 20 mg/kg twice daily or 15 mg/kg 3 times daily for children 13 years of age oradolescents 50 kg 1.戶(hù)使本產(chǎn)品發(fā)表的科研獻(xiàn) Int J Antimicrob Agents. 2019 Dec;54(6):814-819. bioRxiv. 2020 Apr.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFEREN

11、CES1. Sadler BM, Stein DS. Clinical pharmacology and pharmacokinetics of amprenavir. Ann Pharmacother. 2002 Jan;36(1):102-18.2. Esposito V, Verdina A, Manente L, Amprenavir inhibits the migration in human hepatocarcinoma cell and the growth of xenografts. J Cell Physiol. 2013Mar;228(3):640-5.3. Helsley RN, Sui Y, Ai N, Pregnane X Receptor Mediates Dyslipidemia Induced by the HIV Protease Inhibitor Amprenavir in Mice. Mol Pharmacol. 2013Jun;83(6):1190-9.McePdfHeightPage 2 of 3 www.MedChemECaution: Product has not been fully