| Identification | Back Directory | [Name]
2-(3-Bromo-4-methoxyphenyl)-3-[(4-chlorophenyl)sulfonyl]-thiazolidine | [CAS]
313669-88-4 | [Synonyms]
BMS-986122
BMS-986122 >=98% (HPLC)
2-(3-Bromo-4-methoxyphenyl)-3-[(4-chlorophenyl)sulfonyl]-thiazolidine
Thiazolidine, 2-(3-bromo-4-methoxyphenyl)-3-[(4-chlorophenyl)sulfonyl]-
positive,BMS986122,modulator,allosteric,recruitment,β-arrestin,adenylyl,Opioid Receptor,BMS-986122,inhibit,cyclase,Inhibitor,protein | [Molecular Formula]
C16H15BrClNO3S2 | [MDL Number]
MFCD00825276 | [MOL File]
313669-88-4.mol | [Molecular Weight]
448.78 |
| Chemical Properties | Back Directory | [Boiling point ]
567.2±60.0 °C(Predicted) | [density ]
1.586±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble20mg/mL, clear | [form ]
powder | [pka]
-8.81±0.40(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
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 [35S]GTPγS binding in mouse brain membranes[1][2]. | [Biochem/physiol Actions]
BMS-986122 may exhibit an antinociception effect in vivo by increasing the efficiency of Met-enkephalin (met-Enk) to inhibit γ aminobutyric acid (GABA) release in the periaqueductal gray region of the brain. | [IC 50]
μ Opioid Receptor/MOR | [References]
[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. DOI:10.1073/pnas.1300393110
[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. DOI:10.1073/pnas.2000017118
[3] Livingston KE, Alt A, Canals M, Traynor JR. Pharmacologic Evidence for a Putative Conserved Allosteric Site on Opioid Receptors. Mol Pharmacol. 2018;93(2):157-167. DOI:10.1124/mol.117.109561 |
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