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My CartCAS：157212-55-0
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 157212-55-0 |
| Name | Bosentan Monohydrate |
| Molecular Formula | C27H29N5O6S·H2O |
| Molecular Weight | 569.63 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 1592732-453-0 |
| MDL | MFCD09751188 |
| SMILES | O=S(NC1=NC(C2=NC=CC=N2)=NC(OCCO)=C1OC3=CC=CC=C3OC)(C4=CC=C(C(C)(C)C)C=C4)=O.O |
| Target Point | Endothelin Receptor |
| Passage | GPCR & G Protein |
| Background | Bosentan hydrate is a competitive endothelin-1 (ET) antagonist. |
| Biological Activity | Bosentan hydrate 是一种竞争性的 endothelin-1 (ET) 拮抗剂，在人SMC中，作用于 ETA 和 ETB 受体，Ki 分别为 4.7 nM 和 95 nM。[1-3] |
| In Vitro | 波生坦(BOS)竞争性地和特异性地拮抗125I标记的ET-1与人平滑肌细胞(SMC)上的ETA受体和人胎盘细胞上的ETB受体的结合。波生坦对人SMC的ETA受体的体外结合亲和力为4.7nM，对人SMC或胎盘细胞的ETB受体的体外结合亲和力为41或95nM。在体外125I标记试验中，波生坦对ETA的选择性比ETB受体高67倍(平均IC50 = 7.1对474.8 nM)[1]。 |
| In Vivo | 单剂量波生坦62.5 mg(对基线p <0.01)血浆ET-1水平在WHO患者II级或III期特发性或CTD相关PAH的7例患者中显着增加2倍，在8 h达到峰值水平[1]。在高血压大鼠中，当在波生坦100mg / kg之上给予时，Macitentan 30mg / kg进一步降低平均动脉血压(MAP)19mmHg。相反，在Macitentan之上给出的波生坦未能诱导额外的MAP减少。在肺高血压大鼠中，Macitentan 30 mg / kg进一步降低了波生坦顶部4 mm Hg的平均肺动脉压(MPAP)，而在Macitentan上给予的最大有效剂量的波生坦不会导致任何额外的MPAP降低[3] 。 |
| Cell Experiment | 通过台盼蓝排除试验评估细胞活力。用指定浓度的波生坦(10，20和40μM)处理人真皮成纤维细胞。在24和48小时检查细胞活力。用血细胞计数器计数染色(死亡)和未染色(存活)细胞[2]。 |
| Animal Experiment | 大鼠[3]使用2个月大的DSS大鼠和2个月大的Wistar大鼠。平均动脉压(MAP)或平均肺动脉压(MPAP)和心率(HR)的药理学影响在单次强饲后120小时测量，剂量范围为0.1至100 mg/kg(Macitentan)或3至600 mg/kg(波生坦)。为了确定Macitentan是否能提供优于Bosentan的药理活性，设计了一项研究，其中：1)Macitentan在剂量反应曲线建立的波生坦最大有效剂量的基础上给药。 2)在最大有效剂量的Macitentan之上施用相同剂量的波生坦。第二化合物的最大有效剂量以第一测试化合物的Tmax施用。 |
| Data Literature Source | [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 |
| Unit | Bottle |
| Specification | 50mg 10mM*1mL in DMSO 100mg 250mg |
Bosentan hydrate 是一种竞争性的 endothelin-1 (ET) 拮抗剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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