Amprenavir

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

Amprenavir  Chemical Structure

Molecular Weight(MW): 505.63

Amprenavir is a potent PXR-selective agonist, and an HIV protease inhibitor, used to treat HIV.

Size Price Stock Quantity  
In DMSO USD 220 In stock
USD 60 In stock
USD 447 In stock
USD 870 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Purity & Quality Control

Choose Selective HIV Protease Inhibitors

Biological Activity

Description Amprenavir 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

Solubility (25°C)

In vitro Ethanol 100 mg/mL (197.77 mM)
DMSO 16 mg/mL (31.64 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 505.63
Formula

C25H35N3O6S

CAS No. 161814-49-9
Storage powder
in solvent
Synonyms 141W94, VX-478, KVX-478

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01290211 Completed Healthy ViiV Healthcare|Pfizer April 2011 Phase 1
NCT01290211 Completed Healthy ViiV Healthcare|Pfizer April 2011 Phase 1
NCT01209065 Completed Infections Human Immunodeficiency Virus and Herpesviridae ViiV Healthcare|GlaxoSmithKline September 2010 Phase 1
NCT01209065 Completed Infections Human Immunodeficiency Virus and Herpesviridae ViiV Healthcare|GlaxoSmithKline September 2010 Phase 1
NCT01140412 Terminated Healthy ViiV Healthcare|Pfizer July 2010 Phase 1
NCT01140412 Terminated Healthy ViiV Healthcare|Pfizer July 2010 Phase 1

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

HIV Protease Signaling Pathway Map

Related HIV Protease Products0

Tags: buy Amprenavir | Amprenavir supplier | purchase Amprenavir | Amprenavir cost | Amprenavir manufacturer | order Amprenavir | Amprenavir distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID