BMS-707035

SKU: orb1300785

Description

BMS-707035

Research Area

Infectious Disease & Virology, Protein Biochemistry

Key Properties

• CAS Number: 729607-74-3
• MW: 410.42
• Purity: 99.78%
• Formula: C₁₇H₁₉FN₄O₅S
• SMILES: Cn1c(nc(C(=O)NCc2ccc(F)cc2)c(O)c1=O)N1CCCCS1(=O)=O
• Target: HIV Protease
• Solubility: DMSO:36 mg/mL (87.72 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.87 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  HIV-1 integrase:15 nM
• In Vitro:
  BMS-707035 is a pyrimidine carboxamide similar to Raltegravir, the first integrase inhibitor licensed for clinical use. BMS-707035 is a potent, specific, and reversible HIV-I integrase (IN) inhibitor that blocks HIV IN strand transfer activity with IC50 of 15 nM. However, several IN mutations, including V75I, Q148R, V151I, and G163R are found to confer resistance to HIV IN inhibitors. The binding of BMS-707035 and target DNA to IN are mutually exclusive events, as revealed by the fact that the inhibition of strand transfer catalysis by BMS-707035 is overcome by increasing amount of target DNA. The binding affinity of BMS-707035 to IN is also affected by the four terminal bases at the 5' end of the pre-processed U5 long terminal repeat (LTR). Gln148 of IN is crucial for the binding of BMS-707035 to IN. The 3' terminus of the viral LTR, on the other hand, retards the rate of BMS-707035 association with IN, by regulating the kinetics of binding and dissociation.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

phamacokinetics, strand transfer, inhibit, Human immunodeficiency virus, Inhibitor, HIV, HIV Integrase, HIV Protease, HIV-1 integrase strand transfer, HIVProtease, HIV-I integrase, antiviral, BMS707035, BMS-707035, BMS 707035, CYP

Compound Identifiers

PubChem CID

54682040