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Home Cardiovascular Heart Autophagy Pexacerfont - ≥98%(HPLC), high purity , Corticotropin releasing factor receptor 1 antagonist, CAS No.459856-18-9, Corticotropin releasing factor receptor 1 antagonist
Pexacerfont - ≥98%(HPLC), high purity , Corticotropin releasing factor receptor 1 antagonist, CAS No.459856-18-9, Corticotropin releasing factor receptor 1 antagonist
Potent and selective CRF1antagonist; anxiolytic
Basic Description Synonyms PEXACERFONT | 459856-18-9 | BMS-562086 | CRF1 ANTAGONIST | LF1VBG4ZUK | Dpc-a69448 | BMS562086 | N-((R)-sec-butyl)-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine | 8-(6-Methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-N-((1R)-1-methylpropy Specifications & Purity Moligand™, ≥98%(HPLC) Biochemical and Physiological Mechanisms Potent and selective corticotropin-releasing factor 1 receptor (CRF1) antagonist (IC50= 6.1 nM). Displays >150 fold selectivity for CRF1over CRF2b. Inhibits CRF-mediated adrenocorticotropic hormone (ACTH) release from pituitary cell culture (IC50= 129 nM) Storage Temp Store at -20°C Shipped In Ice chest + Ice pads Grade Moligand™ Action Type ANTAGONIST Mechanism of action Corticotropin releasing factor receptor 1 antagonist
Associated Targets(Human) Associated Targets(non-human) Names and Identifiers IUPAC Name N-[(2R)-butan-2-yl]-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine INCHI InChI=1S/C18H24N6O/c1-7-10(2)19-18-22-13(5)21-17-16(12(4)23-24(17)18)14-8-9-15(25-6)20-11(14)3/h8-10H,7H2,1-6H3,(H,19,21,22)/t10-/m1/s1 InChi Key LBWQSAZEYIZZCE-SNVBAGLBSA-N Canonical SMILES CCC(C)NC1=NC(=NC2=C(C(=NN21)C)C3=C(N=C(C=C3)OC)C)C Isomeric SMILES CC[C@@H](C)NC1=NC(=NC2=C(C(=NN21)C)C3=C(N=C(C=C3)OC)C)C PubChem CID 9884366 Molecular Weight 340.43
Chemical and Physical Properties Solubility Solvent:DMSO, Max Conc. mg/mL: 34.04, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 34.04, Max Conc. mM: 100
References 1. Mochizuki M, Kojima T, Kobayashi K, Kotani E, Ishichi Y, Kanzaki N, Nakagawa H, Okuda T, Kosugi Y, Yano T et al. . (2017) Discovery of 4-chloro-2-(2,4-dichloro-6-methylphenoxy)-1-methyl-7-(pentan-3-yl)-1H-benzimidazole, a novel CRF1 receptor antagonist.. Bioorg Med Chem, 25 (5): (1556-1570). [PMID:28174066 ]
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