BMS-986122

BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (μ-OR) . BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [35S]GTPγS binding in mouse brain membranes[1][2].

Product Specifications

CAS Number

[313669-88-4]

UNSPSC

12352005

Hazard Statement

H319

Target

Opioid Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/bms-986122.html

Purity

99.90

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=S(N1C(C2=CC=C(OC)C(Br)=C2)SCC1)(C3=CC=C(Cl)C=C3)=O

Molecular Formula

C16H15BrClNO3S2

Molecular Weight

448.78

Precautions

H319

References & Citations

[1]Burford NT, et al. Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor. Proc Natl Acad Sci U S A. 2013;110 (26) :10830-10835.|[2]Kandasamy R, et al. Positive allosteric modulation of the mu-opioid receptor produces analgesia with reduced side effects. Proc Natl Acad Sci U S A. 2021;118 (16) :e2000017118.|[3]Livingston KE, Alt A, Canals M, Traynor JR. Pharmacologic Evidence for a Putative Conserved Allosteric Site on Opioid Receptors. Mol Pharmacol. 2018;93 (2) :157-167.