Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BMS-378806 (BMS-806) 是一种 HIV-1 抑制剂,可选择性抑制 HIV-1 gp120 结合到 CD4 受体,EC50为 0.85-26.5 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 395 | 现货 | ||
2 mg | ¥ 566 | 现货 | ||
5 mg | ¥ 913 | 现货 | ||
10 mg | ¥ 1,580 | 现货 | ||
25 mg | ¥ 3,130 | 现货 | ||
50 mg | ¥ 4,590 | 现货 | ||
100 mg | ¥ 6,570 | 现货 | ||
500 mg | ¥ 13,200 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 976 | 现货 |
产品描述 | BMS-378806 (BMS-806) selectively inhibits the binding of HIV-1 gp120 to the CD4 receptor with EC50 of 0.85-26.5 nM in virus. |
靶点活性 | CD4-gp120:0.85 nM-26.5 nM(EC50) |
体外活性 | BMS-806, a 7-azaindole derivative, binds gp120 and interferes with the interaction of HIV surface protein gp120 with the host cell receptor CD4. BMS-806 inhibits a panel of macrophage- and T cell-tropic HIV-1 strains, which are laboratory strains that use either CCR5 (M-tropic) or CXR4 (T-tropic) co-receptors to enter cells and are classified as B subtypes. The aqueous solubility from the crystalline form of BMS-806 (BMS 378806) is 170 μg/mL. The solubility of BMS-806 is 1.3 mg/mL at pH=2.1 and 3.3 mg/mL at pH=11, a solubility profile that reveals the amphoteric nature of BMS-806 and estimates the pKa of the protonated form as 2.9 while that of the free base is approximately 9.6. BMS-806 competes with soluble CD4 binding to a monomeric form of gp120 in an ELISA assay with IC50 = ~ 100 nM. BMS-806 is specific towards HIV-1, with no significant inhibitory activity against HIV-2, SIV, MuLV, RSV, HCMV, BVDV, VSV, and influenza virus observed at concentrations ranging from 10 to 30 μM and no overt cytotoxicity toward host cells, CC50 values > 225 μM. [1] BMS-806 binds directly to gp120 at a stoichiometry of approximately 1:1, with a binding affinity similar to that of soluble CD4. The potential BMS-806 target site is localized to a specific region within the CD4 binding pocket of gp120 by using HIV-1 gp120 variants carrying either compound-selected resistant substitutions or gp120-CD4 contact site mutations. [2] |
体内活性 | When BMS-806 is administered dose-proportional increases in the AUC and Cmax is observed. In rat, dog and monkey, plasma levels of drug exceeded the concentrations required to half-maximally inhibit virus replication in vitro. The volume of distribution of BMS-806 ranges from 0.4 to 0.6 L/kg, indicative of partitioning beyond plasma; however, examination of brain levels in the rat revealed minimal CNS penetration. [1] BMS-806 is stable in human, rat, dog and monkey blood at 37 °C during a 2-h incubation. The blood-to-plasma concentration ratios in humans, rats, dogs and monkeys are 1.1, 0.77, 1.2 and 0.92 (n=3), respectively, suggesting that BMS-806 is distributed to approximately the same extent between plasma and blood cells. The human clearance of BMS-806 predicted from microsomes is 9.2 ml/min/kg (46% of the hepatic blood flow). [3] |
激酶实验 | Drug susceptibility Assay: In general, host cells are infected with HIV-1 at a multiplicity of infection (MOI) of 0.005 50% tissue culture infective doses (TCID50)/cell followed by incubation in the presence of serially diluted inhibitors for 4 to 7 days. Virus yields are quantitated using an RT assay or a p24 enzyme-linked immunosorbent assay (ELISA) (NEN). The results from at least three experiments are used to calculate the 50% effective concentrations (EC50s). The EC50s of IDV, SQV, RTV, and NFV are compared to that of BMS-806 using Dunnett's test. These comparisons are made separately within each assay system. Dunnett's test is used to reduce the probability of false-positive results when a number of treatments are being compared to a control. Confidence bounds for the fold increases in EC50s observes when the same drug is tested in two different assay systems are computed using Fieller's theorem. The use of this theorem is necessary because ratios of parameters (in this case, EC50s) are known not to follow a standard probability distribution, such as the normal distribution. Numbers within the confidence interval are not significantly different from the observed fold increase at the 95% level. |
细胞实验 | To determine cytotoxicity, MT-2 cells are incubated in the presence of serially diluted BMS-806 for 6 days and cell viability is quantitated using an XTT [2,3-bis(2-methoxy-4-nitro-5-sulfophenyl-2H-tetrazolium-5-carboxanilide] assay to calculate the 50% cytotoxic concentrations (CC50s). (Only for Reference) |
别名 | BMS378806, BMS-806, 1-[(2R)-4-苯甲酰基-2-甲基-1-哌嗪基]-2-(4-甲氧基-1H-吡咯并[2,3-B]吡啶-3-基)-1,2-乙二酮 |
分子量 | 406.43 |
分子式 | C22H22N4O4 |
CAS No. | 357263-13-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 3 mg/mL (7.38 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 81 mg/mL (199.29 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.4604 mL | 12.3022 mL | 24.6045 mL | 61.5112 mL |
5 mM | 0.4921 mL | 2.4604 mL | 4.9209 mL | 12.3022 mL | |
DMSO | 10 mM | 0.246 mL | 1.2302 mL | 2.4604 mL | 6.1511 mL |
20 mM | 0.123 mL | 0.6151 mL | 1.2302 mL | 3.0756 mL | |
50 mM | 0.0492 mL | 0.246 mL | 0.4921 mL | 1.2302 mL | |
100 mM | 0.0246 mL | 0.123 mL | 0.246 mL | 0.6151 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。
BMS-378806 357263-13-9 Immunology/Inflammation Microbiology/Virology Proteases/Proteasome gp120/CD4 HIV Protease BMS 806 BMS378806 BMS 378806 Human immunodeficiency virus BMS-806 inhibit 1-[(2R)-4-苯甲酰基-2-甲基-1-哌嗪基]-2-(4-甲氧基-1H-吡咯并[2,3-B]吡啶-3-基)-1,2-乙二酮 HIV BMS806 Inhibitor inhibitor