Amprenavir (VX-478)

Catalog No.S1639 Synonyms: 141W94, VX-478, KVX-478

For research use only.

Amprenavir (VX-478, 141W94, KVX-478) is a potent PXR-selective agonist, and an HIV protease inhibitor, used to treat HIV.

Amprenavir (VX-478) Chemical Structure

CAS No. 161814-49-9

Selleck's Amprenavir (VX-478) has been cited by 2 Publications

Purity & Quality Control

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Biological Activity

Description Amprenavir (VX-478, 141W94, KVX-478) is a potent PXR-selective agonist, and an HIV protease inhibitor, used to treat HIV.
Targets
PXR [1] HIV protease [1]
14.6 ng/mL
In vitro

Amprenavir promotes the specific interactions between the nuclear receptor pregnane X receptor (PXR) and the coactivators SRC-1 and PBP. Amprenavir is docked into the high-resolution crystal structure of human PXR in complex with SR12813. Amprenavir occupies all four subpockets, and its hydroxyl group forms a hydrogen bond with Ser247, which is located in the connection region of PXR, to help to position the drug in the optimal orientation inside the receptor. Amprenavir forms direct contacts with one residue on αAF of the PXR activation function-2 (AF-2) surface, Phe429, which may stabilize the active AF-2 conformation of the receptor and contribute to the agonist activity of amprenavir on PXR. Amprenavir induces the expression of bona fide PXR target genes involved in phase I (CYP3A4), phase II (UGT1A1), and phase III (MDR1) metabolism in both HepaRG cells and LS180 cells. [1]

In vivo Amprenavir increases atherogenic LDL cholesterol fractions in WT mice, but not in PXR−/− mice. Amprenavir stimulates expression of known PXR target genes, including CYP3A11, glutathione transferase A1, and MDR1a, in the intestine of WT mice but not in PXR−/− mice. Amprenavir-mediated PXR activation stimulates the expression of both LipF and LipA in the intestine of WT mice, but not in PXR−/− mice, indicating a possible role of intestinal PXR in mediating dietary lipid breakdown and absorption in mammals. [1]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 505.63
Formula

C25H35N3O6S

CAS No. 161814-49-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)CN(CC(C(CC1=CC=CC=C1)NC(=O)OC2CCOC2)O)S(=O)(=O)C3=CC=C(C=C3)N

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01209065 Completed Drug: GSK1349572|Drug: Fosamprenavir|Drug: Ritonavir Infections Human Immunodeficiency Virus and Herpesviridae ViiV Healthcare|GlaxoSmithKline September 2010 Phase 1
NCT00817765 Completed Drug: Posaconazole|Drug: Fosamprenavir|Drug: Ritonavir HIV Infection|Fungal Infection Radboud University Medical Center|GlaxoSmithKline January 2009 Phase 1
NCT00802074 Completed Drug: Raltegravir|Drug: Fosamprenavir|Drug: Ritonavir Healthy Garden State Infectious Disease Associates PA|GlaxoSmithKline December 2008 Not Applicable
NCT00764465 Completed Drug: Maraviroc|Drug: Fosamprenavir|Drug: Ritonavir Healthy Garden State Infectious Disease Associates PA|GlaxoSmithKline October 2008 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-11-29)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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