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S1RA hydrochloride

Catalog No. T4229 CAS 1265917-14-3

Synonyms: E-52862 hydrochloride

S1RA hydrochloride (E-52862 hydrochloride) is an effective and specific sigma-1 receptor(σ1R, Ki: 17 nM) antagonist, and has good selectivity against σ2R (Ki < 1000 nM).

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S1RA hydrochloride, CAS 1265917-14-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 133.00
25 mg	In stock	$ 288.00
50 mg	In stock	$ 450.00
100 mg	In stock	$ 663.00
500 mg	In stock	$ 1,390.00
1 mL * 10 mM (in DMSO)	In stock	$ 93.00

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Purity: 99.78%

Purity: 99.65%

Purity: 99.4%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	S1RA hydrochloride (E-52862 hydrochloride) is an effective and specific sigma-1 receptor(σ1R, Ki: 17 nM) antagonist, and has good selectivity against σ2R (Ki > 1000 nM).
Targets&IC50	σ1:17 nM
In vitro	S1RA showed high affinity for the guinea pig (Ki: 23.5 nM) and human (Ki: 17 nM) σ1 receptors but no marked affinity for 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 at 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).
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 for 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 started the day of surgery. Intrathecal pre-treatment with idazoxan prevented the systemic S1RA antinociceptive effect, suggesting that the S1RA antinociception depends on the activation of spinal α2 -adrenoceptors which, in turn, could induce an inhibition of formalin-evoked glutamate release. When administered locally, intrathecal S1RA inhibited only the flinching behavior, whereas intracerebroventricularly or intraplantarly injected also attenuated the lifting/licking behavior.

Synonyms	E-52862 hydrochloride
Molecular Weight	373.87
Formula	C20H24ClN3O2
CAS No.	1265917-14-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 57 mg/mL

References and Literature

1. Díaz JL, et al. Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862). J Med Chem. 2012 Oct 11;55(19):8211-24. 2. Romero L, et al. Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization. Br J Pharmacol. 2012 Aug;166(8):2289-306. 3. Vidal-Torres A, et al. Effects of the selective sigma-1 receptor antagonist S1RA on formalin-induced pain behavior and neurotransmitter release in the spinal cord in rats. J Neurochem. 2014 Jan 3.

Citations

1. Meng F, Xiao Y, Ji Y, et al. An open-like conformation of the sigma-1 receptor reveals its ligand entry pathway. Nature Communications. 2022, 13(1): 1-11.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library GPCR Compound Library Immunology/Inflammation Compound Library Anti-Metabolism Disease Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library Preclinical Compound Library

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S1R agonist 1 hydrochloride Blarcamesine hydrochloride σ1 Receptor antagonist-1 S1R agonist 2 KB-5492 FA Siramesine 4-PPBP maleate NE-100 hydrochloride

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Keywords

S1RA hydrochloride 1265917-14-3 GPCR/G Protein Sigma receptor Inhibitor E 52862 E 52862 Hydrochloride E52862 S1RA E-52862 E-52862 Hydrochloride E-52862 hydrochloride inhibit S1RA Hydrochloride S-1RA hydrochloride Sigma Receptor E52862 Hydrochloride inhibitor

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