Rel-SB-612111 (hydrochloride)

Rel-SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM) . rel-SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. rel-SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model[1].

Product Specifications

CAS Number

[371980-94-8]

UNSPSC

12352005

Target

Opioid Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/rel-sb-612111-hydrochloride.html

Solubility

10 mM in DMSO

Smiles

O[C@@H]1C[C@H](CN2CCC(C3=C(Cl)C=CC=C3Cl)CC2)CCC4=C(C)C=CC=C41.[H]Cl

Molecular Formula

C24H30Cl3NO

Molecular Weight

454.86

References & Citations

[1]Paola F Zaratin, et al. Modification of Nociception and Morphine Tolerance by the Selective Opiate Receptor-Like Orphan Receptor Antagonist (-) -cis-1-methyl-7-[[4- (2,6-dichlorophenyl) piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111) .J Pharmacol Exp Ther. 2004 Feb;308 (2) :454-61.