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Sigma-1 receptor antagonist 1
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Sigma-1 receptor antagonist 1图片
CAS NO:1639220-19-1
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Sigma?1 receptor antagonist 1 (compound 137) 是一种高效选择性的 sigma-1 受体 (σ1R) 拮抗剂，对 σ1R 具有高亲和力 (Ki = 1.06 nM)。Sigma?1 receptor antagonist 1 具有抗神经痛活性，有作为治疗神经性疼痛药物的前景。
Cas No.1639220-19-1
Canonical SMILESCC1=NC(C2=CC=C(Cl)C=C2)=NC(OCCCN3CCCCC3)=C1Cl
分子式C19H23Cl2N3O
分子量380.31
溶解度DMSO: 6.25 mg/mL (16.43 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Sigma?1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma?1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain[1].

Sigma?1 receptor antagonist 1 exhibits a high binding affinity to σ1R receptor (Ki = 1.06 nM) and good σ-1/2 selectivity (1344-fold)[1].

Sigma?1 receptor antagonist 1 exerts dose-dependent antinociceptive effects in mice formalin model and rats CCI models of neuropathic pain[1].

[1]. Lan Y, et al. Synthesis and biological evaluation of novel sigma-1 receptor antagonists based on pyrimidine scaffold as agents for treating neuropathic pain. J Med Chem. 2014 Dec 26;57(24):10404-23.