1. Anti-infection
    Metabolic Enzyme/Protease
  2. HIV
    HIV Protease
  3. Amprenavir

Amprenavir (Synonyms: VX-478)

Cat. No.: HY-17430 Purity: 99.61%
Handling Instructions

Amprenavir (VX-478) is a HIV protease inhibitor(Ki=0.6 nM) used to treat HIV infection.

For research use only. We do not sell to patients.

Amprenavir Chemical Structure

Amprenavir Chemical Structure

CAS No. : 161814-49-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 67 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
25 mg USD 270 In-stock
Estimated Time of Arrival: December 31
50 mg USD 420 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
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Description

Amprenavir (VX-478) is a HIV protease inhibitor(Ki=0.6 nM) used to treat HIV infection.

IC50 & Target

IC50 Value: 0.6 nM (Ki); Against wild-type clinical HIV isolates:14.6 +/- 12.5 ng/mL (mean +/- SD) [1]. Target: HIV protease

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 [2].

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 [1].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (197.77 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9777 mL 9.8887 mL 19.7773 mL
5 mM 0.3955 mL 1.9777 mL 3.9555 mL
10 mM 0.1978 mL 0.9889 mL 1.9777 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.94 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.94 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.94 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Molecular Weight

505.63

Formula

C₂₅H₃₅N₃O₆S

CAS No.

161814-49-9

SMILES

O=C(O[[email protected]@H]1COCC1)N[[email protected]@H](CC2=CC=CC=C2)[[email protected]](O)CN(S(=O)(C3=CC=C(N)C=C3)=O)CC(C)C

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Amprenavir
Cat. No.:
HY-17430
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Amprenavir

Cat. No.: HY-17430