Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Temsavir (BMS626529) 是一种新型附着抑制剂,靶向 HIV-1 gp120 并阻止其与 CD4+ T 细胞结合。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 325 | 现货 | ||
2 mg | ¥ 462 | 现货 | ||
5 mg | ¥ 863 | 现货 | ||
10 mg | ¥ 1,390 | 现货 | ||
25 mg | ¥ 2,590 | 现货 | ||
50 mg | ¥ 3,860 | 现货 | ||
100 mg | ¥ 5,530 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 889 | 现货 |
产品描述 | Temsavir (BMS626529) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells. |
体外活性 | BMS-626529 has half-maximal effective concentration (EC50) values of <10 nM against the vast majority of viral isolates. BMS-626529 exhibits an average EC50 against LAI virus of 0.7±0.4 nM. BMS-626529 exhibits an EC50 of 0.01 nM against the most susceptible virus and an EC50 of >2,000 nM against the least susceptible virus. The cytotoxicity profile of BMS-626529 is examined in several cell types from different human tissues. CC50 values of >200 μM are observed in MT-2 (T lymphocytes), HEK293 (kidney), HEp-2 (larynx), HepG2 (liver), HeLa (cervix), HCT116 (colorectal), MCF-7 (breast), SK-N-MC (neuroepithelium), HOS (bone), H292 (lung), and MDBK (bovine kidney) cells measured after 3 or 6 days in culture. CC50 values of 105 and 192 μM are obtained in the T-cell line PM1 and in PBMCs, respectively, following 6 days in culture. These results show that BMS-626529 exhibits low cytotoxicity in cell culture[1]. BMS-626529 exhibits a broad spectrum of antiviral activity against a panel of clinical isolates, with a 50% inhibitory concentration (IC50) ranging from subnanomolar levels to >0.1 μM[2]. |
激酶实验 | Micro BioSpin 6 columns are used to measure the binding of [3H]BMS-488043 or [3H]BMS-626529 to gp120. Binding solutions (30 μL) containing 25 mM Tris-HCl (pH 7.5), 125 mM NaCl, 50 nM gp120JRFL, and serial dilutions of [3H]BMS-488043 or [3H]BMS-626529 are allowed to equilibrate and then adsorbed to a MicroBioSpin 6 column. The column is centrifuged (~14,000 rpm) for 5 min, the eluent is collected, and radioactivity is determined with a scintillation counter. To measure dissociative kinetics, 150 nM [3H]BMS-626529 or 90 nM [3H]BMS-488043 is incubated with 60 nM gp120 at ambient temperature for 1 h to achieve equilibrium binding, and then a large molar excess (14-fold) of soluble CD4 protein is added to drive dissociation. Aliquots are taken at the indicated time intervals, adsorbed to a spin column, and centrifuged, and the radioactivity in the eluent is quantitated. Comparison of the tritium signal from parallel samples with and without the soluble CD4 challenge allowed for the determination of the percent compound bound[1]. |
细胞实验 | Cytotoxicity assays are performed in the presence of serially diluted BMS-626529 for up to 6 days, and cell viability is quantitated using an XTT assay. To determine CC50?values (concentration of drug required to kill 50% of cells), laboratory-adapted peripheral blood mononuclear cells (PBMCs) are initially plated at a density of 0.1×106?cells/mL. In the absence of compounds, the cell densities typically reach 1×106?to 1.2×106/mL after 6 days[1]. |
别名 | BMS626529 |
分子量 | 473.48 |
分子式 | C24H23N7O4 |
CAS No. | 701213-36-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 8.57 mg/mL (18.1 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.112 mL | 10.5601 mL | 21.1202 mL | 52.8005 mL |
5 mM | 0.4224 mL | 2.112 mL | 4.224 mL | 10.5601 mL | |
10 mM | 0.2112 mL | 1.056 mL | 2.112 mL | 5.2801 mL |
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。
Temsavir 701213-36-7 Microbiology/Virology Proteases/Proteasome HIV Protease inhibit BMS 626529 BMS626529 Human immunodeficiency virus BMS-626529 Inhibitor HIV inhibitor