A positive allosteric modulator of δ-opioid receptors; has an average EC50 value of 30 nM for β-arrestin recruitment in the presence of the endogenous δ-opioid receptor agonist leu-enkephalin

BMS 986187 – 1 mg

Brand:
Cayman
CAS:
684238-37-7
Storage:
-20
UN-No:
Non-Hazardous - /

BMS 986187 is a positive allosteric modulator of δ-opioid receptors.{38565} In the presence of the endogenous δ-opioid receptor agonist leu-enkephalin, BMS 986187 has an average EC50 value of 30 nM for β-arrestin recruitment, but has little to no activity in the absence of an agonist. It is 100-fold selective for δ- over µ-opioid receptors in the presence of leu-enkephalin and the endogenous µ-opioid receptor agonist endomorphin I, respectively.  

 

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Description

A positive allosteric modulator of δ-opioid receptors; has an average EC50 value of 30 nM for β-arrestin recruitment in the presence of the endogenous δ-opioid receptor agonist leu-enkephalin, but little to no activity in the absence of an agonist; 100-fold selective for δ- over µ-opioid receptors in the presence of endogenous ligands

Formal name: 3,4,5,6,7,9-hexahydro-3,3,6,6-tetramethyl-9-[4-[(2-methylphenyl)methoxy]phenyl]-1H-xanthene-1,8(2H)-dione

Synonyms: 

Molecular weight: 470.6

CAS: 684238-37-7

Purity: ≥98%

Formulation: A crystalline solid

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

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