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S1RA hydrochloride

Cat. No. M28096

All AbMole products are for research use only, cannot be used for human consumption.

S1RA hydrochloride Structure
Synonym:

E-52862 hydrochloride

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Quality Control & Documentation
Biological Activity

S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization.

Chemical Information
Molecular Weight 373.88
Formula C20H24ClN3O2
CAS Number 1265917-14-3
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Water 16.67 mg/mL (ultrasonic)
Storage 4°C, dry, sealed
References

[1] Rafael González-Cano, et al. Pharmacol Res. Urinary bladder sigma-1 receptors: A new target for cystitis treatment

[2] Cristina Sánchez-Fernández, et al. J Pharmacol Exp Ther. Modulation of peripheral μ-opioid analgesia by σ1 receptors

Related Sigma Receptor Products
Siramesine hydrochloride

Siramesine (Lu 28-179) hydrochloride is an effective sigma-2 receptor agonist. Siramesine has a nanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and is 140 times more selective for sigma-2 receptors (IC50=17 nM). Siramesine has xC-system inhibitory activity associated with iron death.

Siramesine

Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes.

S1RA

S1RA (E-52862) is a potent and selective sigma-1 receptor (σ1R, Ki=17 nM), which showes good selectivity against σ2R (Ki > 1000 nM).

Pentoxyverine Citrate

Pentoxyverine citrate is an orally active sigma-1 receptor agonist with Ki values of 41 nM for σ1, 894 nM for σ2, and 75 nM for σ1 in guinea pig brain membranes.Pentoxyverine citrate is also a muscarinic antagonist.

Cutamesine dihydrochloride

Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a novel and selective opioid sigma1 receptor agonist with IC50 of 17.4 nM.

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Keywords: S1RA hydrochloride, E-52862 hydrochloride supplier, Sigma Receptor, inhibitors, activators

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