Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Bosentan (Benzenesulfonamide) 是 endothelin-1 (ET)拮抗剂,在人的 SMC 细胞中,它能够作用于 ETA 受体(Ki:4.7 nM)和 ETB 受体(Ki:95 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
10 mg | ¥ 218 | 现货 | ||
25 mg | ¥ 343 | 现货 | ||
50 mg | ¥ 492 | 现货 | ||
100 mg | ¥ 872 | 现货 | ||
200 mg | ¥ 1,660 | 现货 | ||
500 mg | ¥ 2,560 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 547 | 现货 |
产品描述 | Bosentan (Benzenesulfonamide) is a sulfonamide-derived, competitive and specific endothelin receptor antagonist with a slightly higher affinity for the endothelin A receptor than endothelin B receptor. Bosentan blocks the action of endothelin 1, an extremely potent endogenous vasoconstrictor and bronchoconstrictor, by binding to endothelin A and endothelin B receptors in the endothelium and vascular smooth muscle. Bosentan decreases both pulmonary and systemic vascular resistance and is particularly used in the treatment of pulmonary arterial hypertension. |
靶点活性 | ETB:95 nM(Ki), ETA:4.7 nM(Ki) |
体外活性 | In vitro, bosentan has been shown to improve human endothelial cell and reduce neointimal and smooth muscle proliferation[3]. |
体内活性 | In pigs in vivo, bosentan has been shown to partially restore hypoxia-induced reductions in nitric oxide[3]. |
细胞实验 | Incubation solutions containing bosentan (1, 10 and 100 µM) are prepared in cell culture medium. On the sixth day of culturing of the sandwich-cultured hepatocytes, cell culture medium is removed from the wells and incubation solution containing bosentan is added to the cells. The cells were incubated with the solution for 24 h at 37°C. After the exposure, the incubation solution id removed and the cells are rinsed with Plus (+) or Minus (−) buffer. The buffer solution is then removed and the cells are incubated with fresh Plus (+) or Minus (−) buffer for 5 min at 37°C. Following this 5 minute incubation, the buffer solution is collected and any remaining buffer is removed. The cells are then washed three times with ice-cold Plus (+) buffer and the plates are frozen at −80°C until processed for bioanalysis. (Only for Reference) |
别名 | Actelion, 波生坦, Ro 47-0203, Benzenesulfonamide |
分子量 | 551.614 |
分子式 | C27H29N5O6S |
CAS No. | 147536-97-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 3 mg/mL (5.43 mM)
DMSO: 100 mg/mL (181.28 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.8129 mL | 9.0643 mL | 18.1286 mL | 45.3215 mL |
5 mM | 0.3626 mL | 1.8129 mL | 3.6257 mL | 9.0643 mL | |
DMSO | 10 mM | 0.1813 mL | 0.9064 mL | 1.8129 mL | 4.5322 mL |
20 mM | 0.0906 mL | 0.4532 mL | 0.9064 mL | 2.2661 mL | |
50 mM | 0.0363 mL | 0.1813 mL | 0.3626 mL | 0.9064 mL | |
100 mM | 0.0181 mL | 0.0906 mL | 0.1813 mL | 0.4532 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。
Bosentan 147536-97-8 GPCR/G Protein Endothelin Receptor Actelion 波生坦 Ro 47-0203 Inhibitor inhibit Benzenesulfonamide inhibitor