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    Amprenavir
    Amprenavir

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem 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. In addition, it is reported to be a Cytochrome P450 3A4 Inhibitor. Amprenavir has been effectively used for the treatment of HIV disease in patients with primary HIV infection. It was approved by the FDA on April 15, 1999, for twice-a-day dosing instead of needing to be taken every eight hours. 

    References: Mol Pharmacol. 2013 Jun;83(6):1190-9.

    Related CAS:226700-79-4 (Fosamprenavir, Amprenavir phosphate; GW 433908); 226700-81-8 (Fosamprenavir calcium salt; Lexiva; GW433908G; GW-908)

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    Molecular Weight (MW)505.63
    FormulaC25H35N3O6S
    CAS No.161814-49-9 (Amprenavir); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (197.8 mM)
    Water: <1 mg/mL
    Ethanol: 16 mg/mL (31.6 mM)
    Other infoChemical Name: [(3S)-oxolan-3-yl] N-[(2S,3R)-4-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamate
    InChi Key: YMARZQAQMVYCKC-UHFFFAOYSA-N
    InChi Code: InChI=1S/C25H35N3O6S/c1-18(2)15-28(35(31,32)22-10-8-20(26)9-11-22)16-24(29)23(14-19-6-4-3-5-7-19)27-25(30)34-21-12-13-33-17-21/h3-11,18,21,23-24,29H,12-17,26H2,1-2H3,(H,27,30)
    SMILES Code: CC(C)CN(CC(C(CC1=CC=CC=C1)NC(=O)OC2CCOC2)O)S(=O)(=O)C3=CC=C(C=C3)N
    Synonyms141W94, VX-478, KVX-478; VX 478; VX478; Agenerase; Prozei; KVX 478; KVX478; Amprenavir;


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    In Vitro

    In vitro activity: 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.


    Cell Assay: Amprenavir induced PXR target gene expression in both HepaRG hepatoma cells and LS180 intestinal cells.

    In VivoAmprenavir 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. 
    Animal modelWT and PXR-/- mice 
    Formulation & Dosage10 mg/kg; p.o.
    ReferencesMol Pharmacol. 2013 Jun;83(6):1190-9.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    Amprenavir

     

    Amprenavir

     

    Amprenavir

    Amprenavir is a potent PXR-selective agonist. Mol Pharmacol. 2013 Jun;83(6):1190-9. 

    Amprenavir

    Key residues of PXR LBD are required for amprenavir’s agonistic activity. Mol Pharmacol. 2013 Jun;83(6):1190-9. 

    Amprenavir

    Amprenavir elicits hyperlipidemia in WT, but not in PXR−/− mice. Mol Pharmacol. 2013 Jun;83(6):1190-9. 
     

    Amprenavir

    Amprenavir elevates atherogenic LDL cholesterol levels in WT mice. Mol Pharmacol. 2013 Jun;83(6):1190-9. 


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