For research use only.
Catalog No.S1639 Synonyms: 141W94, KVX-478
CAS No. 161814-49-9
Amprenavir (VX-478, 141W94, KVX-478) is a potent PXR-selective agonist, and an HIV protease inhibitor, used to treat HIV.
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Choose Selective HIV Protease Inhibitors
|Description||Amprenavir (VX-478, 141W94, KVX-478) is a potent PXR-selective agonist, and an HIV protease inhibitor, used to treat HIV.|
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. 
|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. |
|In vitro||DMSO||16 mg/mL (31.64 mM)|
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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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|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|
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