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

μ Opioid Receptor^[1][3]

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].

366.22

C₁₅H₉Cl₂N₃O₂S

313671-26-0

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