GRADE & PURITYMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.10mM in DMSO
Moligand™, 10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Descripción general
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
Especificaciones y pureza
Moligand™, 10mM in DMSO
Mecanismos bioquímicos y fisiológicos
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
Condiciones de almacenamiento de almacenamiento
Store at -80°C
Enviado en
Dry ice packs + Cold packs
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