S1RA, Selective sigma-1 antagonist (TBI4201)

Description

Product Details

Formal Name: 4-{2-[5-Methyl-1-(napthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine hydrochloride

Alternate Names: E-52862 HCl

Molecular Formula: C₂₀H₂₃N₃O₂·HCl

Formula Weight: 373.88

CAS Number: 1265917-14-3

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

 

Applications

Selective sigma-1 antagonist

 

Functions

S1RA (E-52862) is a potent and selective σ1 antagonist with weak binding at σ2 (IC50’s:  σ1 = 17nM, σ2 = 9300nM). S1RA abolished mechanical and thermal hyperalgesia in mice with carrageenan-induced acute inflammation by enhancing the action of endogenous opioid peptides of immune origin in a σ1 dependent manner. BD1063 potentiated µ-opioid antinociception in mice in a σ-dependent manner. S1RA displayed neuroprotective effects in a mouse model of ischemic stroke.

 

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Additional information

SIZE (mg)	25 MG, 5 MG

Datasheet:

TBI4201_S1RA

MSDS:

TBI4201_S1RA_MSDS_2024