Pexacerfont

Pexacerfont is an antagonist of corticotropin-releasing factor receptor 1 (CRF1, IC50 = 6.1 nM for the human receptor). It is selective for CRF1 in IMR-32 cells (mean IC50 = 10.6 nM) over CFR2beta receptors endogenously expressed in pig choroid plexus membranes (IC50 = >1,000 nM) in radioligand binding assays and does not bind to the human CRF binding protein (IC50 = >1,000 nM). Pexacerfont inhibits adrenocorticotropic hormone (ACTH) release induced by CRF in primary rat pituitary cells with an IC50 value of 129 nM. It increases the time spent in the open arms of the elevated plus maze (EPM) in rats, indicating anxiolytic-like activity, when administered at doses ranging from 10 to 30 mg/kg.Formal Name: 8-(6-methoxy-2-methyl-3-pyridinyl)-2,7-dimethyl-N-[(1R)-1-methylpropyl]-pyrazolo[1,5-a]-1,3,5-triazin-4-amine. CAS Number: 459856-18-9. Synonyms: BMS 562086, DPC-A69448. Molecular Formula: C18H24N6O. Formula Weight: 340.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 30 mg/ml, Ethanol: 30 mg/ml. lambdamax: 283 nm. SMILES: CC1=NN(C(N[C@H](C)CC)=NC(C)=N2)C2=C1C3=C(N=C(C=C3)OC)C. InChi Code: 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.