Efaroxan (hydrochloride)

Efaroxan is an alpha2-adrenergic receptor (alpha2-AR, EC50s = 1 receptor antagonist. It binds to alpha2A-, alpha2B-, and alpha2C-ARs (Kis = 13, 38, and 1,820 nM, respectively) and selectively to I1 over I2 receptors (Kis = 52 and >10,000 nM, respectively). Efaroxan is an I3 agonist that binds to putative I3 receptors on human pancreatic islets of Langerhans and stimulates insulin secretion when used at a concentration of 100 µM. It also binds to rat RIN-5AH insulinoma cell membranes (IC50 = 32 nM) and stimulates insulin secretion when used at a concentration of 100 µM. Efaroxan (5 mg/kg) lowers basal blood glucose levels in mice. It also increases 3,4-dihydroxyphenylalanine (L-DOPA, Cay-13248) synthesis in rat cortex and hippocampus by 77 and 57%, respectively, when administered at a dose of 10 mg/kg.Formal Name: 2-(2-ethyl-2,3-dihydro-2-benzofuranyl)-4,5-dihydro-1H-imidazole, monohydrochloride. CAS Number: 89197-00-2. Synonyms: (±)-Efaroxan, RX 821037. Molecular Formula: C13H16N2O . HCl. Formula Weight: 252.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 15mg/ml, DMSO: 10mg/ml, Ethanol: 10mg/ml, PBS (pH 7.2): 10mg/ml. lambdamax: 216, 277, 283 nm. SMILES: CCC1(C2=NCCN2)CC3=CC=CC=C3O1.Cl. InChi Code: InChI=1S/C13H16N2O.ClH/c1-2-13(12-14-7-8-15-12)9-10-5-3-4-6-11(10)16-13,/h3-6H,2,7-9H2,1H3,(H,14,15),1H. InChi Key: DWOIUCRHVWIHAH-UHFFFAOYSA-N.