Amprenavir

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Chemical Structure| 161814-49-9 同义名 : 安普那韦 ;VX-478; APV; Agenerase; Prozei; KVX-478; 141W94
CAS号 : 161814-49-9
货号 : A375111
分子式 : C25H35N3O6S
纯度 : 99%+
分子量 : 505.63
MDL号 : MFCD00934214
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(207.66 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • HIV Protease

    HIV protease, IC50:14.6 ng/mL
描述 Amprenavir is a selective HIV protease inhibitor with a Ki value of 0.6nM. The IC50 value of amprenavir against wild-type clinical HIV isolates in vitro is 14.6 ± 12.5ng/mL.[3] Treatment of Huh-7 cells with amprenavir (50μM) significantly inhibited invasion, blocked the conversion of latent MMP-2 to its 62/64-kD active form, but had no effect on cell proliferation compared to the DMSO-treated controls. Treatment with amprenavir via intragastric gavage (60 mg/kg/d, 5 days/week) for 3 weeks delayed tumor growth in nude mice inoculated with hepatoma Huh-7 cells.[4]
作用机制 Amprenavir prevents the virally encoded HIV protease from processing the cleavage of its natural substrates, gag and gag-pol polyproteins. It exerts the antiretroviral effect late in the HIV life cycle by interfering with virion maturation.[3]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.89mL

1.98mL

0.99mL

19.78mL

3.96mL

1.98mL
参考文献

[1]Helsley RN, Sui Y, et al. Pregnane X receptor mediates dyslipidemia induced by the HIV protease inhibitor amprenavir in mice. Mol Pharmacol. 2013 Jun;83(6):1190-9.

[2]Fung HB, Kirschenbaum HL, Hameed R. Amprenavir: a new human immunodeficiency virus type 1 protease inhibitor. Clin Ther. 2000 May;22(5):549-72.

[3]Sadler BM, Stein DS. Clinical pharmacology and pharmacokinetics of amprenavir. Ann Pharmacother. 2002 Jan;36(1):102-18

[4]Esposito V, Verdina A, Manente L, Spugnini EP, Viglietti R, Parrella R, Pagliano P, Parrella G, Galati R, De Luca A, Baldi A, Montesarchio V, Chirianni A. Amprenavir inhibits the migration in human hepatocarcinoma cell and the growth of xenografts. J Cell Physiol. 2013 Mar;228(3):640-5