Fostemsavir Tris

SKU: orb1219369

Description

Fostemsavir Tris is the prodrug of BMS-626529,is a oral, safe and effective inhibitor of HIV-1 attachment. It inhibits human immunodeficiency virus type 1 (HIV-1) infection by binding to gp120 and interfering with the attachment of virus to CD4+ T-cells.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 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. (In Vivo):Fostemsavir Tris has good antiviral activity in subjects infected with virus shown to be susceptible (IC50, <100 nM) to the agent.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 864953-39-9
• MW: 704.62
• Purity: >98% (HPLC)
• 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
• Solubility: DMSO:125 mg/mL (177.40 mM; Need ultrasonic); H2O:100 mg/mL (141.92 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  Fostemsavir Tris has good antiviral activity in subjects infected with virus shown to be susceptible (IC50, <100 nM) to the agent.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BMS-663068 Tris,FOSTEMSAVIR TROMETHAMINE

Quick Database Links

Gene Symbol

HIV