| Name | BMS-707035 |
| Description | BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2. |
| 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. [1] 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. [1] 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. [2] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 36 mg/mL (87.72 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.87 mM), Sonication is recommended.
|
| Keywords | strand transfer | phamacokinetics | Inhibitor | inhibit | Human immunodeficiency virus | HIVProtease | HIV-I integrase | HIV-1 integrase strand transfer | HIV Protease | HIV Integrase | HIV | CYP | BMS-707035 | BMS707035 | BMS 707035 | antiviral |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Emtricitabine | Dolutegravir intermediate-1 | Dimethyl fumarate | Lamivudine | Chloroquine phosphate | Valproic Acid | (-)-Epigallocatechin Gallate | Decanedioic acid | Dextran sulfate sodium salt (MW 5000) | Tenofovir |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Drug Repurposing Compound Library | Anti-Viral Compound Library | Inhibitor Library | PPI Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Preclinical Compound Library | Anti-COVID-19 Compound Library | Human Metabolite Library |
United States
