Aformoterol is the (R,R)-enantiomer of the β2-adrenergic receptor (β2-AR) agonist formoterol.
| Cas No. | 200815-49-2 |
| 别名 | 酒石酸福莫特罗; (R,R)-Formoterol tartrate |
| Canonical 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 |
| 分子式 | C19H24N2O4•C4H6O6 |
| 分子量 | 494.5 |
| 溶解度 | DMF: 12.5 mg/ml,DMSO: 25 mg/ml,PBS (pH 7.2): 2.5 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Aformoterol is the (R,R)-enantiomer of the β2-adrenergic receptor (β2-AR) agonist formoterol . It selectively binds to β1- over β2-ARs (Kds = 2.9 and 113 nM, respectively) as well as β3-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 , 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). |
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