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BMS-986121

Names

[ CAS No. ]:
313671-26-0

[ Name ]:
BMS-986121

Biological Activity

[Description]:

BMS-986121 is a positive allosteric modulator (PAM) of the μ opioid receptor extracted from patent WO2014107344. BMS-986121 is built on a chemical scaffold representing a new chemotype for μ receptor PAMs[1][2][3].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Opioid Receptor
Signaling Pathways >> Neuronal Signaling >> Opioid Receptor
Research Areas >> Neurological Disease

[Target]

μ Opioid Receptor[1][3]


[In Vitro]

BMS-986121 (1 μM~1 mM) significantly augments the β-arrestin–recruitment response produced by a low concentration of endomorphin-I (PAM-detection mode). BMS-986121 significantly increases the inhibition of forskolin-stimulated adenylyl cyclase activity produced by a ∼EC10 (30 pM) concentration of endomorphin-I in CHOμ cells. BMS-986121 (100 μM) produces leftward shifts in the potency of endomorphin-I (fourfold), morphine (fivefold), and leu-enkephalin (sixfold), in inhibition of forskolin-stimulated cAMP-accumulation assays in CHO-μ cells[1].

[References]

[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]. WO2014107344

[3]. Bisignano P, et al. Ligand-Based Discovery of a New Scaffold for Allosteric Modulation of the μ-Opioid Receptor. J Chem Inf Model. 2015;55(9):1836-1843.

Chemical & Physical Properties

[ Molecular Formula ]:
C15H9Cl2N3O2S

[ Molecular Weight ]:
366.22


Related Compounds