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Bosentan hydrate

CAS No. : 157212-55-0

MCE 站：Bosentan hydrate

产品活性：Bosentan hydrate 是一种竞争性的 endothelin-1 (ET) 拮抗剂，在人SMC中，作用于 ET_A 和 ET_B 受体，K_i 分别为 4.7 nM 和 95 nM。

研究领域：GPCR/G Protein

作用靶点：Endothelin Receptor

In Vitro: Bosentan (BOS) competitively ａnd specifically antagonizes binding of ¹²⁵I-labelled ET-1 to ET_A receptors on human smooth muscle cells (SMC) ａnd ET_B receptors on human placenta cells. The in vitro binding affinity of Bosentan to ET_A receptors on human SMC is 4.7 nM ａnd to ET_B receptors on human SMC or placenta cells is 41 or 95 nM. Bosentan has 67-fold greater selectivity for ET_A than ET_B receptors (mean IC₅₀=7.1 vs 474.8 nM) in an in vitro ¹²⁵I-labeling assay.

In Vivo: In hypertensive rats, Macitentan 30 mg/kg further decreases mean arterial blood pressure (MAP) by 19 mm Hg when given on top of Bosentan hydrate 100 mg/kg. Conversely, Bosentan hydrate 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 hydrate, whereas a maximal effective dose of Bosentan hydrate given on top of Macitentan does not cause any additional MPAP decrease.

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