A positive allosteric modulator of μ-opioid receptors (EC50 = 3 μM for endomorphin 1-stimulated β-arrestin recruitment in U2OS-OPRM1 cells expressing human μ-opioid receptors); potentiates endomorphin 1-induced inhibition of forskolin-stimulated adenylyl cyclase activity in CHO cells expressing human μ-opioid receptors (EC50 = 8.9 μM); enhances DAMGO-stimulated [35S]GTPγ binding in C6μ glioma cell membranes and mouse brain membranes

BMS 986122 – 1 mg

Brand:
Cayman
CAS:
313669-88-4
Storage:
-20
UN-No:
Non-Hazardous - /

BMS 986122 is a positive allosteric modulator of μ-opioid receptors that increases β-arrestin recruitment stimulated by endomorphin 1 (Item No. 23280) in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors (EC50 = 3 μM).{37687} It 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 also enhances [35S]GTPγ binding stimulated by the μ-opioid agonist DAMGO (Item No. 21553) by 7- and 4.5-fold in C6μ glioma cell membranes that express μ-opioid receptors and mouse brain membranes, respectively.  

 

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SKU: 23269 - 1 mg Category:

Description

A positive allosteric modulator of μ-opioid receptors (EC50 = 3 μM for endomorphin 1-stimulated β-arrestin recruitment in U2OS-OPRM1 cells expressing human μ-opioid receptors); potentiates endomorphin 1-induced inhibition of forskolin-stimulated adenylyl cyclase activity in CHO cells expressing human μ-opioid receptors (EC50 = 8.9 μM); enhances DAMGO-stimulated [35S]GTPγ binding in C6μ glioma cell membranes and mouse brain membranes

Formal name: 2-(3-bromo-4-methoxyphenyl)-3-[(4-chlorophenyl)sulfonyl]-thiazolidine

Synonyms: 

Molecular weight: 448.8

CAS: 313669-88-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Research Area|Neuroscience

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