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Cat #: V0733 CAS #: 161814-49-9 Purity ≥ 98%
Description: Amprenavir (formerly VX-478; trade name Agenerase and Prozei), an FDA approved drug for treating HIV infections, is a potent PXR-selective agonist, and an HIV protease inhibitor with the IC50 of 0.6 nM on HIV-1 protease, it also weakly inhibits HIV-2 protease with IC50 value of 19 nM.
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Molecular Weight (MW) | 505.63 |
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Molecular Formula | C25H35N3O6S |
CAS No. | 161814-49-9 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 100 mg/mL (197.8 mM)r |
Water: <1 mg/mLr | |
Ethanol: 16 mg/mL (31.6 mM) | |
SMILES Code | CC(C)CN(CC(C(CC1=CC=CC=C1)NC(=O)OC2CCOC2)O)S(=O)(=O)C3=CC=C(C=C3)N |
Synonyms | 141W94, VX-478, KVX-478; VX 478; VX478; Agenerase; Prozei; KVX 478; KVX478; Amprenavir; |
Protocol | In Vitro | Amprenavir has an enzyme inhibition constant (Ki = 0.6 nM) that falls within the Ki range of the other protease inhibitors. Amprenavir's in vitro 50% inhibitory concentration (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 cell lines, inhibiting MMP proteolytic activation. |
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In Vivo | Amprenavir was able to promote regression of hepatocarcinoma growth 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 and induced PXR target gene expression in vitro and in vivo. Short-term exposure to amprenavirsignificantly increased plasma 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 capsule doses are 1200 mg twice daily for adults and 20 mg/kg twice daily or 15 mg/kg 3 times daily for children < 13 years of age or adolescents < 50 kg. |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.9777 mL | 9.8887 mL | 19.7773 mL | 39.5546 mL |
5mM | 0.3955 mL | 1.9777 mL | 3.9555 mL | 7.9109 mL |
10mM | 0.1978 mL | 0.9889 mL | 1.9777 mL | 3.9555 mL |
20mM | 0.0989 mL | 0.4944 mL | 0.9889 mL | 1.9777 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.