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 |
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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. |