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首页-小分子抑制剂&激动剂-GPCR-Endothelin Receptor-Pipersentan
Pipersentan

Chemical Structure : Pipersentan

CAS No.: 2305865-93-2

Pipersentan (Diosuxentan)

货号: PC-25043Not For Human Use, Lab Use Only.

Pipersentan (Diosuxentan) is a potent, selective endothelin receptor A (ETA receptor) antagonist, inhibits binding of 125I-ET-1 toward recombinant ETA receptor with IC50 of 4.44 nM, >1000-fold selective over ETB receptor.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Pipersentan (Diosuxentan) is a potent, selective endothelin receptor A (ETA receptor) antagonist, inhibits binding of 125I-ET-1 toward recombinant ETA receptor with IC50 of 4.44 nM, >1000-fold selective over ETB receptor.
Pipersentan completely inhibits the high intracellular calcium induced by ET-1 in recombinant CHO and SK-N-MC cells with IC50 of 1.6 nM, >30,000-fold selective over ET B.
Pipersentan efficaciously antagonized the effects of ET-1 on pulmonary artery smooth muscle cell proliferation, migration and calcium mobilization and effectively improved right ventricular hypertrophy and pulmonary arterial pressure in both monocrotaline- and hypoxia-induced pulmonary hypertension (PH) rat models.

物理化学性质&存储条件

分子量 569.39
分子式 C20H21BrN6O7S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Sulfamide, N-[5-(1,3-benzodioxol-5-yl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N′-(2-methoxyethyl)-

参考文献

1. Zeyu Zhang, et al. Front Pharmacol. 2022 Jun 20:13:920222.

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