Sigma-1 receptor antagonist 1_product_DataBase

Bioactivity

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].

Target

Ki: 1.06 nM (σ1R)

Invitro

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].

In Vivo

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

Name

Sigma-1 receptor antagonist 1

CAS

1639220-19-1

Formula

C19H23Cl2N3O

Molar Mass

380.31

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.

PeptideDB

Sigma-1 receptor antagonist 1

CAS: 1639220-19-1 F: C19H23Cl2N3O W: 380.31