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BMS-986121

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Catalog No. T40392Cas No. 313671-26-0

BMS-986121, a positive allosteric modulator (PAM) of the μ opioid receptor. This compound is based on a novel chemical scaffold, introducing a new chemotype for μ receptor PAMs.

BMS-986121

BMS-986121

😃Good
Catalog No. T40392Cas No. 313671-26-0
BMS-986121, a positive allosteric modulator (PAM) of the μ opioid receptor. This compound is based on a novel chemical scaffold, introducing a new chemotype for μ receptor PAMs.
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Product Introduction

Bioactivity
Description
BMS-986121, a positive allosteric modulator (PAM) of the μ opioid receptor. This compound is based on a novel chemical scaffold, introducing a new chemotype for μ receptor PAMs.
In vitro
BMS-986121, at concentrations ranging from 1 μM to 1 mM, significantly enhances the β-arrestin recruitment response initiated by a low level of endomorphin-I (PAM-detection mode). It also markedly boosts the suppression of forskolin-induced adenylyl cyclase activity by a near-EC10 concentration (30 pM) of endomorphin-I in CHOμ cells. Furthermore, at 100 μM, BMS-986121 elevates the efficacy of endomorphin-I (fourfold), morphine (fivefold), and leu-enkephalin (sixfold) in reducing forskolin-stimulated cAMP accumulation in CHO-μ cells[1].
Chemical Properties
Molecular Weight366.22
FormulaC15H9Cl2N3O2S
Cas No.313671-26-0
Relative Density.1.530 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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