Sigma-1 receptor antagonist 1 

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 (K_i = 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 (K_i = 1.06 nM) and good σ-1/2 selectivity (1344-fold)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

380.31

C₁₉H₂₃Cl₂N₃O

1639220-19-1

Solid

Light yellow to yellow

CC1=NC(C2=CC=C(Cl)C=C2)=NC(OCCCN3CCCCC3)=C1Cl

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]