For research use only. Not for therapeutic Use.
BMS-986121 is a positive allosteric modulator (PAM) of the μ opioid receptor extracted from patent WO2014107344. BMS-986121 is built on a chemical scaffold representing a new chemotype for μ receptor PAMs[1][2][3].
BMS-986121 (1 μM~1 mM) significantly augments the β-arrestin–recruitment response produced by a low concentration of endomorphin-I (PAM-detection mode). BMS-986121 significantly increases the inhibition of forskolin-stimulated adenylyl cyclase activity produced by a ∼EC10 (30 pM) concentration of endomorphin-I in CHOμ cells. BMS-986121 (100 μM) produces leftward shifts in the potency of endomorphin-I (fourfold) and leu-enkephalin (sixfold), in inhibition of forskolin-stimulated cAMP-accumulation assays in CHO-μ cells[1].
| Catalog Number | I045273 |
| CAS Number | 313671-26-0 |
| Synonyms | N-(2,6-dichlorophenyl)-4-(4-nitrophenyl)-1,3-thiazol-2-amine |
| Molecular Formula | C15H9Cl2N3O2S |
| Purity | ≥95% |
| InChI | InChI=1S/C15H9Cl2N3O2S/c16-11-2-1-3-12(17)14(11)19-15-18-13(8-23-15)9-4-6-10(7-5-9)20(21)22/h1-8H,(H,18,19) |
| InChIKey | AOCLKIVPDLQCOF-UHFFFAOYSA-N |
| SMILES | C1=CC(=C(C(=C1)Cl)NC2=NC(=CS2)C3=CC=C(C=C3)[N+](=O)[O-])Cl |
| Reference | [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. [2]. WO2014107344 [3]. Bisignano P, et al. Ligand-Based Discovery of a New Scaffold for Allosteric Modulation of the μ-Opioid Receptor. J Chem Inf Model. 2015;55(9):1836-1843. |
