Indacaterol

Indacaterol is a long-acting and selective beta2-adrenergic receptor (beta2-AR) agonist (EC50 = 8.71 nM for increasing intracellular cAMP levels in vitro). It is selective for beta2-ARs over beta1- and beta3-ARs (Kis = 43.6, 616.6, and 3,311.3 nM, respectively). Indacaterol inhibits bronchoconstriction induced by serotonin (5-HT, Cay-14332) in conscious guinea pigs with a maximal effect of 85% when administered intratracheally at a dose of 6.7 µg/kg. It also inhibits bronchoconstriction induced by methacholine (Cay-23092) in rhesus monkeys with a maximal effect of 75% when administered via nebulization at a dose of 12.5 mg/kg. Formulations containing indacaterol have been used alone, and in combination with glycopyrrolate, in the treatment of chronic obstructive pulmonary disease.Formal Name: 5-[(1R )-2-[(5,6-diethyl-2,3-dihydro-1H-inden-2-yl)amino]-1-hydroxyethyl]-8-hydroxy 2(1H )-quinolinone. CAS Number: 312753-06-3. Synonyms: QAB149. Molecular Formula: C24H28N2O3. Formula Weight: 392.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml, DMSO: 15 mg/ml, Ethanol: 1 mg/ml. lambdamax: 260, 281, 292 nm. SMILES: O[C@H](C1=C(C=CC(N2)=O)C2=C(O)C=C1)CNC3CC4=CC(CC)=C(CC)C=C4C3. InChi Code: InChI=1S/C24H28N2O3/c1-3-14-9-16-11-18(12-17(16)10-15(14)4-2)25-13-22(28)19-5-7-21(27)24-20(19)6-8-23(29)26-24/h5-10,18,22,25,27-28H,3-4,11-13H2,1-2H3,(H,26,29)/t22-/m0/s1. InChi Key: QZZUEBNBZAPZLX-QFIPXVFZSA-N.