CAS NO: | 147536-97-8 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
1 g | 电议 |
5 g | 电议 |
生物活性 | Bosentan is a competitive and dual antagonist ofendothelin-1 (ET)for theETAandETBreceptors withKiof 4.7 nM and 95 nM in human SMC, respectively. | ||||||||||||||||
IC50& Target | Ki: 4.7 nM (ETAreceptor, in human SMC), 95 nM (ETAreceptor, in human SMC)[1] | ||||||||||||||||
体外研究 (In Vitro) | Bosentan (BOS) competitively and specifically antagonizes binding of125I-labelled ET-1 to ETAreceptors on human smooth muscle cells (SMC) and ETBreceptors on human placenta cells. The in vitro binding affinity of Bosentan to ETAreceptors on human SMC is 4.7 nM and to ETBreceptors on human SMC or placenta cells is 41 or 95 nM. Bosentan has 67-fold greater selectivity for ETAthan ETBreceptors (mean IC50=7.1 vs 474.8 nM) in an in vitro125I-labeling assay[1]. | ||||||||||||||||
体内研究 (In Vivo) | Single-dose Bosentan 62.5 mg significantly (p<0.01 vs baseline) plasma ET-1 levels by 2-fold in 7 pts with WHO class II or III idiopathic or CTD-associated PAH, with peak levels achieved at 8 h[1]. In hypertensive rats, Macitentan 30 mg/kg further decreases mean arterial blood pressure (MAP) by 19 mm Hg when given on top of Bosentan 100 mg/kg. Conversely, Bosentan given on top of Macitentan fails to induce an additional MAP decrease. In pulmonary hypertensive rats, Macitentan 30 mg/kg further decreases mean pulmonary artery pressure (MPAP) by 4 mm Hg on top of Bosentan, whereas a maximal effective dose of Bosentan given on top of Macitentan does not cause any additional MPAP decrease[3]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 551.61 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C27H29N5O6S | ||||||||||||||||
CAS 号 | 147536-97-8 | ||||||||||||||||
中文名称 | 伯森坦;柏森坦;波生坦 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(181.29 mM) *"≥" means soluble, but saturation unknown. 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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