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sigma-1 Receptor antagonist 1

  Cat. No.:  DC60319   Featured
Chemical Structure
1639220-19-1
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Field of application
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].
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1639220-19-1
Chemical Name: sigma-1 Receptor antagonist 1
Synonyms: BDBM50034090;5-Chloro-2-(4-chlorophenyl)-4-methyl-6-(3-(piperidin-1-yl)propoxy)pyrimidine
SMILES: ClC1=C(C([H])([H])[H])N=C(C2C([H])=C([H])C(=C([H])C=2[H])Cl)N=C1OC([H])([H])C([H])([H])C([H])([H])N1C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H]
Formula: C19H23Cl2N3O
M.Wt: 380.3114
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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)[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].
In Vitro: 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].
References: [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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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