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Sigma-1 receptor antagonist 3

CAS: 1639220-17-9 F: C19H23ClFN3O W: 363.86

Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (σ1) receptor antagonist with a Ki of 1.1
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Bioactivity Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (σ1) receptor antagonist with a Ki of 1.14 nM. Sigma-1 receptor antagonist 3 inhibits Human Ether-a-go-go-Related Gene (hERG) with an IC50 of 1.54 μM. Sigma-1 receptor antagonist 3 has the potential for the neuropathic pain[1].
Target IC50: 1.54μM (hERG). Ki : 1.14 nM (Sigma-1 receptor); 1239 nM (Sigma-2 receptor)
Name Sigma-1 receptor antagonist 3
CAS 1639220-17-9
Formula C19H23ClFN3O
Molar Mass 363.86
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Reference [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.