Sigma-1 receptor antagonist 1 |
Catalog No.GC38038 |
시그마-1 수용체 길항제 1(화합물 137)은 강력하고 선택적인 시그마-1 수용체(σ1R) 길항제로, σ1R 수용체(Ki = 1.06nM)에 대한 높은 결합 친화도를 가지고 있습니다.
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Cas No.: 1639220-19-1
Sample solution is provided at 25 µL, 10mM.
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.
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