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Icalcaprant

Chemical Structure : Icalcaprant

CAS No.: 2227384-17-8

Icalcaprant (CVL-354, CVL354)

货号: PC-23099Not For Human Use, Lab Use Only.

Icalcaprant (CVL-354) is a potent, selective kappa opioid receptor (KOR) antagonist with Ki of 1.47 nM and IC50 of 0.042 nM, 31-fold binding affinity selectivity over MOR.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Icalcaprant (CVL-354) is a potent, selective kappa opioid receptor (KOR) antagonist with Ki of 1.47 nM and IC50 of 0.042 nM, 31-fold binding affinity selectivity over MOR.
Icalcaprant (CVL-354) blocks KOR-mediated motivational deficits in mice, dose-dependently reverses the suppression of progressive ratio responding induced by spiradoline.
CVL-354 dose-dependently reverses KOR and MOR-induced thermal analgesia.

物理化学性质&存储条件

分子量 406.49
分子式 C23H26N4O3
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

4-[4-[[(2S)-2-(3-Methoxy-1-methyl-1H-pyrazol-4-yl)-1-pyrrolidinyl]methyl]phenoxy]benzamide

参考文献

1. Patent WO2018096510 A1 2018-05-31.

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