Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK812397 is a potent entry inhibitor of X4-tropic strains of HIV-1, as demonstrated in multiple in vitro cellular assays. GSK812397 is a noncompetitive antagonist of the CXCR4 receptor, with GSK812397 producing a concentration-dependent decrease in both an SDF-1-mediated chemotaxis and intracellular calcium release (IC50s were 0.34+/-0.01 nM and 2.41+/-0.50 nM, respectively). GSK812397 is effective against a broad range of X4- and X4R5-utilizing clinical isolates. The potency and efficacy of GSK812397 are dependent on the individual isolate, with complete inhibition of infection observed with 24 of 30 isolates. GSK812397 does not show any detectable in vitro cytotoxicity and was highly selective for CXCR4. GSK812397 shows acceptable pharmacokinetic properties and bioavailability across species. GSK812397 has antiviral activity against a broad range of X4-utilizing strains of HIV-1 via a noncompetitive antagonism of the CXCR4 receptor.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | GSK812397 is a potent entry inhibitor of X4-tropic strains of HIV-1, as demonstrated in multiple in vitro cellular assays. GSK812397 is a noncompetitive antagonist of the CXCR4 receptor, with GSK812397 producing a concentration-dependent decrease in both an SDF-1-mediated chemotaxis and intracellular calcium release (IC50s were 0.34+/-0.01 nM and 2.41+/-0.50 nM, respectively). GSK812397 is effective against a broad range of X4- and X4R5-utilizing clinical isolates. The potency and efficacy of GSK812397 are dependent on the individual isolate, with complete inhibition of infection observed with 24 of 30 isolates. GSK812397 does not show any detectable in vitro cytotoxicity and was highly selective for CXCR4. GSK812397 shows acceptable pharmacokinetic properties and bioavailability across species. GSK812397 has antiviral activity against a broad range of X4-utilizing strains of HIV-1 via a noncompetitive antagonism of the CXCR4 receptor. |
分子量 | 420.55 |
分子式 | C24H32N6O |
CAS No. | 878197-98-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GSK812397 878197-98-9 GSK 812397 GSK-812397 GSK 812397. Inhibitor inhibitor inhibit