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首页-小分子抑制剂&激动剂-GPCR-Endothelin Receptor-IRL-2500
IRL-2500

Chemical Structure : IRL-2500

CAS No.: 169545-27-1

IRL-2500 (IRL2500, IRL 2500)

货号: PC-23819Not For Human Use, Lab Use Only.

IRL-2500 (IRL 2500) is a potent and selective endothelin-B receptor (ETB) antagonist, inhibits binding of [125I]-endothelin-1 (ET-1) to human ETB with IC50 of 1.3 nM, 70-fold selective over ETA receptor.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

IRL-2500 (IRL 2500) is a potent and selective endothelin-B receptor (ETB) antagonist, inhibits binding of [125I]-endothelin-1 (ET-1) to human ETB with IC50 of 1.3 nM, 70-fold selective over ETA receptor.
IRL 2500 inhibited the sarafotoxin S6c (STX6c)-mediated contraction of the dog saphenous vein (pKb 7.77) and the STX6c-induced relaxation of the preconstricted rabbit mesenteric artery (pKb 6.92)
IRL 2500 (10 mg/kg, i.v.) inhibited the initial transient decrease in mean arterial pressure (MAP) induced by the ETB-selective agonist IRL 1620 (0.5 nmol/kg, i.v.) in anesthetized rats.
IRL 2500 (10 mg/kg, i.v.) inhibited the initial transient decrease in mean arterial pressure (MAP) induced by the ETB-selective agonist IRL 1620 (0.5 nmol/kg, i.v.).

物理化学性质&存储条件

分子量 573.69
分子式 C36H35N3O4
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

((R)-3-([1,1'-Biphenyl]-4-yl)-2-(N,3,5-trimethylbenzamido)propanoyl)-L-tryptophan

参考文献

1. Balwierczak JL, et al. J Cardiovasc Pharmacol. 1995;26 Suppl 3:S393-6.

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