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]:
[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]
[2]. WO2014107344
Chemical & Physical Properties
[ Molecular Formula ]:
C15H9Cl2N3O2S
[ Molecular Weight ]:
366.22