Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM). However, it has no effect on CCR5-using (R5) viruses. AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells. 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 AMD 3465 hexahydrobromide 的水溶性和稳定性通常比游离态更好。
产品描述 | AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM). However, it has no effect on CCR5-using (R5) viruses. AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells. |
靶点活性 | HIV-2 (ROD):12.3 nM (in MT-4 cells), X4 HIV-1 (HE):9.8 nM (in MT-4 cells), X4 HIV-1 (RF):7.4 nM (in MT-4 cells), X4 HIV-1 (IIIB):12.3 nM (in MT-4 cells), 12G5 mAb-CXCR4:0.75 nM (in SupT1 cells), CXCL12 (AF647)-CXCR4:18 nM (in SupT1 cells), X4 HIV-1 (NL4.3):6.1 nM (in MT-4 cells), X4 HIV-1 (NL4.3AMD3100):2822 nM (in MT-4 cells), HIV-2 (EHO):12.3 nM (in MT-4 cells) |
体外活性 | AMD 3465 is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells and it is cytotoxic to the X4 HIV-1 strains IIIB, NL4.3, RF and HE with an IC50 ranging from 6 to 12 nM. AMD 3465 inhibits CXCL-12-induced growth in U87 and Daoy cells. AMD 3465 treatment stimulates the phosphorylation of Erk1/2 in U87 and Daoy cells[2]. AMD 3465 (50 nM) totally blocks CXCL12-induced calcium mobilization, with an IC50 of 17 nM. However, it shows no effect on the intracellular calcium fluxes elicited by the CCR5 ligands RANTES, LD78β and MIP-1β in U87.CD4.CCR5 cells. AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses. The IC50 for suppression of the HIV-2 strains ROD and EHO is 12.3 nM[1]. |
体内活性 | AMD 3465 (2.5 mg/kg/d, s.c. for 5 weeks) significantly blocks the growth of U87 GBM and Daoy xenografts[2]. |
别名 | GENZ-644494 |
分子量 | 410.6 |
分子式 | C24H38N6 |
CAS No. | 185991-24-6 |
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。
AMD 3465 185991-24-6 Microbiology/Virology Proteases/Proteasome HIV Protease AMD3465 GENZ 644494 GENZ644494 AMD-3465 GENZ-644494 Inhibitor inhibitor inhibit