AM6545

Peripherally-restricted cannabinoid receptor 1 (CB1) selective antagonists have the potential to inhibit food intake while also escaping centrally-mediated neuropsychiatric side effects. AM6545 is a novel CB1 selective neutral antagonist with low CNS penetration, exhibiting Ki values of 1.7 and 523 nM for CB1 and CB2 receptors, respectively. It reduces food intake and food-reinforced behavior, such as time spent feeding, in a dose-dependent manner, resulting in decreased body weight. AM6545 produces improvements in glucose homeostasis, fatty liver, and plasma lipid profiles in mice with diet-induced obesity. It does not affect behavior responses that are associated with activation of CB1 receptors in the brain.Formal Name: 5-[4-(4-cyano-1-butyn-1-yl)phenyl]-1-(2,4-dichlorophenyl)-N-(1,1-dioxido-4-thiomorpholinyl)-4-methyl-1H-pyrazole-3-carboxamide. CAS Number: 1245626-05-4. Molecular Formula: C26H23Cl2N5O3S. Formula Weight: 556.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml. lambdamax: 268 nm. SMILES: ClC1=CC(Cl)=C(N2N=C(C(NN3CCS(CC3)(=O)=O)=O)C(C)=C2C4=CC=C(C#CCCC#N)C=C4)C=C1. InChi Code: InChI=1S/C26H23Cl2N5O3S/c1-18-24(26(34)31-32-13-15-37(35,36)16-14-32)30-33(23-11-10-21(27)17-22(23)28)25(18)20-8-6-19(7-9-20)5-3-2-4-12-29/h6-11,17H,2,4,13-16H2,1H3,(H,31,34). InChi Key: XBHQLFVDGLPBCK-UHFFFAOYSA-N.