Arformoterol (tartrate)

Aformoterol is the (R,R)-enantiomer of the beta2-adrenergic receptor (beta2-AR) agonist formoterol (Cay-15584). It selectively binds to beta1- over beta2-ARs (Kds = 2.9 and 113 nM, respectively) as well as beta3-adrenergic, B2 bradykinin, neurokinin 1 (NK1) and NK2 receptors when used at concentrations up to 3 µM. Aformoterol induces cAMP accumulation in cultured human bronchial epithelial cells. Ex vivo, aformoterol (0.01-1,000 nM) induces dose-dependent relaxation of guinea pig tracheal strips precontracted with carbamoylcholine (Cay-14486), ovalbumin, or histamine (pD2s = 8.4, 9.5, and 9.5, respectively). In vivo, aformoterol reverses histamine- and ovalbumin-induced bronchoconstriction in guinea pigs (ED50s = 1 and 40 nmol/kg, respectively). Formulations containing aformoterol have been used in the treatment of chronic obstructive pulmonary disease (COPD).Formal Name: N-[2-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]phenyl]-formamide, (2R,3R)-2,3-dihydroxybutanedioate. CAS Number: 200815-49-2. Synonyms: (R,R)-Formoterol. Molecular Formula: C19H24N2O4 . C4H6O6. Formula Weight: 494.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 12.5 mg/ml, DMSO: 25 mg/ml, PBS (pH 7.2): 2.5 mg/ml. lambdamax: 216, 247, 284 nm. SMILES: COC1=CC=C(C[C@@H](C)NC[C@H](O)C2=CC(NC=O)=C(O)C=C2)C=C1.OC([C@H](O)[C@@H](O)C(O)=O)=O. InChi Code: InChI=1S/C19H24N2O4.C4H6O6/c1-13(9-14-3-6-16(25-2)7-4-14)20-11-19(24)15-5-8-18(23)17(10-15)21-12-22,5-1(3(7)8)2(6)4(9)10/h3-8,10,12-13,19-20,23-24H,9,11H2,1-2H3,(H,21,22),1-2,5-6H,(H,7,8)(H,9,10)/t13-,19+,1-,2-/m11/s1. InChi Key: FCSXYHUNDAXDRH-OKMNHOJOSA-N.