S1RA

SKU: orb1223765

Description

A potent and selective sigma-1 receptor antagonist with Ki of 17 nM; shows excellent selectivity over sigma-2 receptor (Ki>1 uM); shows high activity in the mouse capsaicin model of neurogenic pain, exerts dose-dependent antinociceptive effects in several neuropathic pain models.Pain Phase 2 Clinical.

Key Properties

• CAS Number: 878141-96-9
• MW: 337.4155
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₃N₃O₂
• SMILES: CC1=CC(OCCN2CCOCC2)=NN1C1=CC2=CC=CC=C2C=C1
• Target: Sigma receptor
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Animal model: WT and TRPA1 KO mice with AITC (10 μl at 10 mM) in their hind paws. Dosage: 40 mg/kg. Administration: IP; single dose; 24-h before evaluation. Result: Produced a substantial reduction in pain-related responses to intradermal AITC in WT mice.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

E-52862

Quick Database Links

Gene Symbol

Sigma receptor