Fostemsavir Tris

SKU: orb1309917

Description

Fostemsavir Tris (BMS-663068 Tris) is an oral prodrug of the active attachment inhibitor BMS-626529. It blocks HIV-1 infection by binding to viral gp120, preventing its attachment to host CD4+ T-cells. This mechanism has been validated in both in vitro antiviral assays and in vivo clinical research for antiretroviral therapy.

Research Area

Infectious Disease & Virology, Pharmacology & Drug Discovery, Protein Biochemistry

Key Properties

• CAS Number: 864953-39-9
• MW: 704.62
• Purity: 99.45% (May vary between batches)
• Formula: C₂₉H₃₇N₈O₁₁P
• SMILES: O=C(N1CCN(C(C2=CC=CC=C2)=O)CC1)C(C3=CN(COP(O)(O)=O)C4=C3C(OC)=CN=C4N5N=C(C)N=C5)=O.OCC(CO)(N)CO
• Target: HIV Protease
• Solubility: H2O:100 mg/mL (141.92 mM);DMSO:125 mg/mL (177.4 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (5.68 mM)

Bioactivity

• In Vivo:
  BMS-663068 is the phosphonooxymethyl prodrug of BMS-626529, a novel small-molecule attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4(+) T cells.The activity of BMS-626529 is virus dependent, due to heterogeneity within gp120. BMS-626529 had half-maximal effective concentration (EC(50)) values of <10 nM against the vast majority of viral isolates; however, susceptibility varied by >6 log(10), with half-maximal effective concentration values in the low pM range against the most susceptible viruses. The in vitro antiviral activity of BMS-626529 was generally not associated with either tropism or subtype, with few exceptions. Measurement of the binding affinity of BMS-626529 for purified gp120 suggests that a contributory factor to its inhibitory potency may be a relatively long dissociative half-life.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BMS663068, BMS-663068, BMS-663068 Tris, BMS 663068, inhibit, Inhibitor, HIV, HIV Protease, HIV-1, HIVProtease, Fostemsavir, Fostemsavir Tris, Human immunodeficiency virus

Compound Identifiers

PubChem CID

46892186