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Bosentan
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Bosentan图片
CAS NO:147536-97-8
包装与价格:
包装价格(元)
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
波生坦
Benzenesulfonamide
Actelion
Ro 47-0203
产品介绍
Bosentan 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)。

产品描述

Bosentan 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.

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)

Cas No.

147536-97-8

分子式

C27H29N5O6S

分子量

551.62

别名

波生坦;Benzenesulfonamide;Actelion;Ro 47-0203

储存和溶解度

DMSO:100 mg/mL (181.28 mM)
H2O:<1 mgml
Ethanol:3 mg/mL (5.43 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years