BMS 986122

BMS 986122 is a positive allosteric modulator of µ-opioid receptors that increases beta-arrestin recruitment stimulated by endomorphin 1 (Cay-23280) in U2OS-OPRM1 human osteosarcoma cells expressing µ-opioid receptors (EC50 = 3 µM). 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]GTPgamma binding stimulated by the µ-opioid agonist DAMGO (Cay-21553) by 7- and 4.5-fold in C6µ glioma cell membranes that express µ-opioid receptors and mouse brain membranes, respectively.Formal Name: 2-(3-bromo-4-methoxyphenyl)-3-[(4-chlorophenyl)sulfonyl]-thiazolidine. CAS Number: 313669-88-4. Molecular Formula: C16H15BrClNO3S2. Formula Weight: 448.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 2 mg/ml. lambdamax: 234 nm. SMILES: COC1=CC=C(C2N(S(C3=CC=C(Cl)C=C3)(=O)=O)CCS2)C=C1Br. InChi Code: InChI=1S/C16H15BrClNO3S2/c1-22-15-7-2-11(10-14(15)17)16-19(8-9-23-16)24(20,21)13-5-3-12(18)4-6-13/h2-7,10,16H,8-9H2,1H3. InChi Key: PNGJPVDGZNPZHY-UHFFFAOYSA-N.