S1RA hydrochloride

SKU: orb1303040

Description

S1RA hydrochloride (E-52862 hydrochloride) is a potent and selective sigma-1 receptor (σ1R) antagonist with a Ki of 17 nM, demonstrating over 1000-fold selectivity versus the σ2R. This tool compound is widely used in preclinical research to investigate σ1R function in models of neuropathic pain, neurodegenerative diseases, and psychiatric disorders.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1265917-14-3
• MW: 373.87
• Purity: 99.65%
• Formula: C₂₀H₂₄ClN₃O₂
• SMILES: Cl.Cc1cc(OCCN2CCOCC2)nn1-c1ccc2ccccc2c1
• Target: Sigma receptor,5-HT Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.35 mM);DMSO:50 mg/mL (133.74 mM)

Bioactivity

• Target IC50:
  σ1 receptor:17 nM
• In Vivo:
  Control (non-operated) and nerve-injured mice received a Single or repeated (b.i.d, for 12 days) S1RA (25 mg/kg, i.p.) the same dose used fo the assessment of behavioral hypersensitivity in the chronic treatment study. in the behavioral studies, acute treatment was given on day 12 post-surgery and repeated treatment with S1RA starte the day of surgery. Intrathecal pre-treatment with idazoxan prevente the systemic S1RA antinociceptive effect, suggesting tha the S1RA antinociception depends o the activation of spinal α2 -adrenoceptors which, in turn, could induce an Inhibition of formalin-evoked glutamate release. When administered locally, intrathecal S1RA inhibited onl the flinching behavior, whereas intracerebroventricularly or intraplantarly injected also attenuate the lifting/licking behavior.
• In Vitro:
  S1RA showed high affinity fo the guinea pig (Ki: 23.5 nM) and human (Ki: 17 nM) σ1 receptors but no marked affinity fo the σ2 receptors (Ki > 1000 nM for guinea pig and rat σ2 receptors). Moderate affinity (Ki: 328 nM) and antagonistic activity with very low potency IC50 4700 nM) were found a the human 5 hT2B receptor. S1RA showed a low affinity (Ki > 1 μM, IC50 1 μM) for Other additional 170 targets (transporters, receptors, ion channels and enzymes).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

E 52862, E 52862 Hydrochloride, E52862, E-52862, E52862 Hydrochloride, E-52862 Hydrochloride, E-52862 hydrochloride, inhibit, Inhibitor, S1RA, S1RA hydrochloride, S1RA Hydrochloride, S-1RA hydrochloride, Sigmareceptor, Sigma Receptor, Sigma receptor, σ2

Compound Identifiers

PubChem CID

50914801