BMS-986122 - Moligand™, 10mM in DMSO , Allosteric modulator of μ receptor, CAS No.313669-88-4, Allosteric modulator of μ receptor

CAS: 313669-88-4 Cat. No.: B655915 分子式: C₁₆H₁₅BrClNO₃S₂ 分子量: 448.78 EC番号: 806-217-4 PubChem CID: 4644453

GRADE & PURITY Moligand™, 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

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 [ 35 S]GTPγS binding in mouse brain membranes.

In Vitro

BMS-986122 increases β-arrestin recruitment stimulated by endomorphin 1 (EC 50 =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 (EC 50 =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. BMS-986122 increases the potency of Met-Enk to inhibit GABA release in the periaqueductal gray, an important site for antinociception. BMS-986122 is selective for µ-OR and has no detectable activity at the closely related δ-OR. BMS-986122 is a silent allosteric modulator at δ-OR and κ-OR. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Specifications

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

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 pote

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

アクションタイプ

ALLOSTERIC MODULATOR

作用メカニズム

Allosteric modulator of μ receptor

名前と識別子

異性体SMILES

COC1=C(C=C(C=C1)C2N(CCS2)S(=O)(=O)C3=CC=C(C=C3)Cl)Br

WGKドイツ

3

PubChem CID

4644453

分子量

448.78

関連ターゲット（人間）

OPRM1 Tclin Mu-type opioid receptor (2 Activities)

Discover Target: OPRM1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)