BMS-986122 是一种选择性的、有效的μ-阿片受体 (µ-OR) 正变构调节剂。BMS-986122 显示正构激动剂介导的 β-抑制蛋白募集、腺苷酸环化酶抑制和 G 蛋白活化的增强作用。BMS-986122 增强 DAMGO 介导的 [³⁵S]GTPγS 在小鼠脑膜中的结合。

BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (μ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [S]GTPγS binding in mouse brain membranes.

Solid

BMS-986122 increases β-arrestin recruitment stimulated by endomorphin 1 (EC50=3 μM) in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors. BMS-986122 potentiates endomorphin 1-induced inhibition of forskolin-stimulated adenylyl cyclase activity in CHO cells expressing human recombinant μ-opioid receptors (EC50=8.9 μM). BMS-986122 potentiates DAMGO-mediated [35S]GTPγS binding in mouse brain membranes and appears to be, at least in part, a positive affinity modulator of the μ-opioid receptor for DAMGO binding.
BMS-986122 enhances the ability of the endogenous opioid Methionine-enkephalin (Met-Enk) to stimulate G protein activity in mouse brain homogenates without activity on its own and to enhance G protein activation to a greater extent than β-arrestin recruitment in CHO cells expressing human mu-opioid receptors.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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]. Kandasamy R, et al. Positive allosteric modulation of the mu-opioid receptor produces analgesia with reduced side effects. Proc Natl Acad Sci U S A. 2021;118(16):e2000017118.

In Vitro: DMSO : 100 mg/mL (222.83 mM; Need ultrasonic)配制储备液