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首页-小分子抑制剂&激动剂-GPCR-Bradykinin Receptor-ELN441958
ELN441958

Chemical Structure : ELN441958

CAS No.: 913064-47-8

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ELN441958 (ELN-441958)

货号: PC-26908Not For Human Use, Lab Use Only.

ELN441958 is a potent, selective Bradykinin B1 receptor (B1R) antagonist with Ki of 0.26 nM, highly selective for B1 over B2 receptors.

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5 mg ￥980 In stock
10 mg ￥1480 In stock
25 mg ￥2580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ELN441958 is a potent, selective Bradykinin B1 receptor (B1R) antagonist with Ki of 0.26 nM, highly selective for B1 over B2 receptors.
ELN441958 is up to 120-fold more potent at primate than at rodent B1 receptors.
ELN441958 potently antagonized DAKD (but not bradykinin)-induced calcium mobilization in IMR-90 cells.
ELN441958 dose-dependently reduced carrageenan-induced thermal hyperalgesia in a rhesus monkey tail-withdrawal model, with an ED50 ∼3 mg/kg s.c. in primate pain model.

物理化学性质&存储条件

分子量 501.03
分子式 C29H29ClN4O2
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

7-Chloro-2-(3-(9-(pyridin-4-yl)-3,9-diazaspiro[5.5]undecane-3-carbonyl)phenyl)isoindolin-1-one

参考文献

1. Hawkinson JE, et al. J Pharmacol Exp Ther. 2007 Aug;322(2):619-30.

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