| CAS |
No.157212-55-0 |
| 中文名称 |
波生坦一水合物(10mM in DMSO,无菌） |
| 英文名称 |
Bosentan Monohydrate(10mM in DMSO，Sterile） |
| 分子式 |
C27H29N5O6S·H2O |
| 分子量 |
569.63 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 靶点 |
Endothelin Receptor |
| 通路 |
GPCR & G Protein |
| 背景说明 |
Bosentan hydrate 是一种竞争性的 endothelin-1 (ET) 拮抗剂。 |
| 生物活性 |
Bosentan hydrate is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC， respectively.[1-3] |
| IC50 |
Ki: 4.7 nM (ETA receptor， in human SMC)， 95 nM (ETA receptor， in human SMC)[1] |
| In Vitro |
Bosentan (BOS) hydrate 竞争性和特异性拮抗125I 标记的 ET-1 与人平滑肌细胞 (SMC) 上 ETA 受体和人胎盘细胞上 ETB 受体的结合。Bosentan hydrate 与人 SMC 上的 ETA 受体的体外结合亲和力为 4.7 nM，与人 SMC 或胎盘细胞上的 ETB 受体的亲和力为 41 或 95 nM。在体外 125I-标记检测[1]。 |
| In Vivo |
在高血压大鼠中，在 Bosentan hydrate 100 mg/kg 的基础上给予 30 mg/kg 的 Macitentan (HY-14184) 进一步降低平均动脉血压 (MAP=19 mm Hg)。相反，在 Macitentan 之上给予 Bosentan hydrate 不能诱导 MAP 的进一步降低。在肺动脉高压大鼠中，Macitentan 30 mg/kg在 Bosentan hydrate 的基础上进一步降低平均肺动脉压 (MPA=4 mm Hg)，而在 Macitentan 的基础上给予 Bosentan hydrate 的最大有效剂量不引起任何额外的 MPAP 降低[3]。 |
| 细胞实验 |
Cell viability is evaluated by the trypan blue exclusion test. Human dermal fibroblasts are treated with the indicated concentration of Bosentan (10， 20 and 40 μM). Cell viability is examined at 24 and 48 hours. Stained (dead) and unstained (viable) cells are counted with a hematocytometer[2]. |
| 动物实验 |
Rats[3] Two-month-old DSS rats and two-month-old Wistar rats are used. Pharmacological effects on mean arterial pressure (MAP) or mean pulmonary arterial pressure (MPAP) and heart rate (HR) are measured up to 120 h after a single gavage at doses ranging from 0.1 to 100 mg/kg (Macitentan) or 3 to 600 mg/kg (Bosentan). To determine whether Macitentan can provide superior pharmacological activity vs. Bosentan， a study is designed in which: 1) Macitentan is administered on top of the maximal effective dose of Bosentan established by the dose-response curve. 2) the same dose of Bosentan is administered on top of the maximal effective dose of Macitentan. The maximal effective dose of the second compound is administered at Tmax of the first tested compound. |
| 数据来源文献 |
[1]. Dhillon S， et al. Bosentan: a review of its use in the management of mildly symptomatic pulmonary arterial hypertension. Am J Cardiovasc Drugs. 2009;9(5):331-50.
[2]. Akamata K， et al. Bosentan reverses the pro-fibrotic phenotype of systemic sclerosis dermal fibroblasts via increasing DNA binding ability of transcription factor Fli1. Arthritis Res Ther. 2014 Apr 3;16(2):R86.
[3]. Iglarz M， et al. Comparison of pharmacological activity of macitentan and bosentan in preclinical models of systemic and pulmonary hypertension. Life Sci. 2014 Nov 24;118(2):333-9. |
| 规格 |
0.1ml 0.3ml 0.5ml 1ml 1.5ml |
| 单位 |
瓶 |
中文
英语
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