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Amprenavir (VX-478)

Name: Amprenavir (VX-478)
Brand: Selleck Chemicals
SKU: S1639
Rating: 5 (3 reviews)

Synonyms: 141W94, VX-478, KVX-478

Catalog No.S1639 Purity: 99.99%

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: 161814-49-9

Selleck's Amprenavir (VX-478) has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 99.99%

99.99

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Signaling Pathway

HIV Protease Signaling Pathway

Choose Selective HIV Protease Inhibitors

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
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
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]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT01209065	Completed	Infections Human Immunodeficiency Virus and Herpesviridae	ViiV Healthcare\|GlaxoSmithKline	September 2010	Phase 1
NCT00817765	Completed	HIV Infection\|Fungal Infection	Radboud University Medical Center\|GlaxoSmithKline	January 2009	Phase 1
NCT00802074	Completed	Healthy	Garden State Infectious Disease Associates PA\|GlaxoSmithKline	December 2008	Not Applicable
NCT00764465	Completed	Healthy	Garden State Infectious Disease Associates PA\|GlaxoSmithKline	October 2008	Phase 2

References

[1] Helsley RN, et al. Mol Pharmacol,?013, 83(6), 1190-1199.

Chemical Information & Solubility

Molecular Weight	505.63	Formula	C₂₅H₃₅N₃O₆S
CAS No.	161814-49-9	SDF	Download Amprenavir (VX-478) SDF
Smiles	CC(C)CN(CC(C(CC1=CC=CC=C1)NC(=O)OC2CCOC2)O)S(=O)(=O)C3=CC=C(C=C3)N
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

Ethanol : 101 mg/mL

DMSO : 30 mg/mL ( (59.33 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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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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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