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编 号:F757338
分子式:C15H9Cl2N3O2S
分子量:366.22
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1mg
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5mg
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10mg
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25mg
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50mg
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生物活性:
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.

体外研究:
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) and leu-enkephalin (sixfold), in inhibition of forskolin-stimulated cAMP-accumulation assays in CHO-μ cells.
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