S1RA (C007B-273334)

InformationS1RA S1RA (E-52862) is a selective sigma-1 receptor (σ1R) antagonist with a reported binding affinity of Ki = 17.0 ± 7.0 nM for human σ1 receptor , selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels.Targetsσ1R 17 nM(Ki)In vitroS1RA behaves as a highly selective σ1 receptor antagonist. It shows high affinity for human (Ki= 17 nM) and guinea pig (Ki= 23.5 nM) σ1 receptors but no significant affinity for the σ2 receptors (Ki > 1000 nM for guinea pig and rat σ2 receptors). It has moderate affinity (Ki= 328 nM) and antagonistic activity, with very low potency (IC50= 4700 nM) against human 5-HT2B receptor. S1RA shows no significant affinity (Ki > 1 µM or % inhibition at 1 µM < 50%) for other additional 170 targets (receptors, transporters, ion channels and enzymes).In vivoS1RA crosses the blood-brain barrier and binds to σ1 receptors in the CNS. Specification: 10mM in DMSO Molecular Formula: C2OH23N3O2 Molecular Weight: 337.42 PubChem CID: 44247568 Isomeric SMILES: CC1=CC(=NN1C2=CC3=CC=CC=C3C=C2)OCCN4CCOCC4