BMS-986121

Modify Date: 2024-01-14 19:43:47

BMS-986121 Structure
BMS-986121 structure
Common Name BMS-986121
CAS Number 313671-26-0 Molecular Weight 366.22
Density N/A Boiling Point N/A
Molecular Formula C15H9Cl2N3O2S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of BMS-986121


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].

 Names

Name BMS-986121

 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
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