卡博特韦 T6098

Product Introduction
Bioactivity


英文名: Cabotegravir

描述: Cabotegravir (S/GSK1265744) 是一种HIV 整合酶抑制剂，可研究艾滋病。它抑制OAT1 和OAT3，IC50值为 0.81 和0.41 μM。

激酶实验: In vitro strand transfer assay: The inhibitory concentrations of GSK1265744 is measured in a strand transfer assay using recombinant HIV IN. A complex of integrase and biotinylated donor DNA–streptavidin-coated SPA beads is formed by incubating 2 μM purified recombinant integrase with 0.66 μM biotinylated donor DNA–4 mg/mL streptavidin-coated SPA beads in 25 mM sodium MOPS pH 7.2, 23 mM NaCl, and 10 mM MgCl2 for 5 minutes at 37°C. These beads are spun down and preincubated with diluted INSTIs for 60 minutes at 37°C. Next, [3H]-labeled target DNA substrate is added to give a final concentration of 7 nM substrate, and the strand transfer reaction is incubated at 37°C for 25 to 45 minutes, which allowed for a linear increase in strand transfer of donor DNA to radiolabeled target DNA. The signal is read using a Wallac MicroBeta scintillation plate reader.

体内活性: GSK1265744（50 mg/kg）可防止高剂量SHIV感染恒河猴.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 36 mg/mL (88.8 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: Human immunodeficiency virus | Cabotegravir | inhibit | HIV Integrase | GSK-744 | UGT1A1 | OAT | GSK 1265744 | HIV | S/GSK-1265744 | Inhibitor | AIDS | antiretroviral | GSK1265744 | GSK 744 | S/GSK 1265744

相关产品: Atazanavir sulfate | (Rac)-Telinavir | Sennoside A | GPI-1046 | BMS-488043 | Doxorubicin hydrochloride | UC-781 | BI 224436 | Opaviraline | Bictegravir

相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Fluorochemical Library | Human Metabolite Library | Inhibitor Library | Pediatric Drug Library | EMA Approved Drug Library | Orally Active Compound Library | NO PAINS Compound Library | Anti-Infection Compound Library

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