CAS NO: | 43229-80-7 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 402.40 |
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Formula | C19H24N2O4.1/2C4H4O4 |
CAS No. | 43229-80-7 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 80 mg/mL (198.8 mM) |
Water: <1 mg/mL | |
Ethanol: <1 mg/mL | |
Other info | Chemical Name: (E)-but-2-enedioic acid;N-[2-hydroxy-5-[(1R)-1-hydroxy-2-[[(2R)-1-(4-methoxyphenyl)propan-2-yl]amino]ethyl]phenyl]formamide InChi Key: OBRNDARFFFHCGE-QDSVTUBZSA-N InChi Code: InChI=1S/2C19H24N2O4.C4H4O4/c2*1-13(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;5-3(6)1-2-4(7)8/h2*3-8,10,12-13,19-20,23-24H,9,11H2,1-2H3,(H,21,22);1-2H,(H,5,6)(H,7,8)/b;;2-1+/t2*13-,19+;/m11./s1 SMILES Code: C[C@H](CC1=CC=C(C=C1)OC)NC[C@@H](C2=CC(=C(C=C2)O)NC=O)O.C[C@H](CC1=CC=C(C=C1)OC)NC[C@@H](C2=CC(=C(C=C2)O)NC=O)O.C(=C/C(=O)O)\C(=O)O |
Synonyms | Eformoterol, CGP 25827A, NSC 299587, YM 08316; Formoterol Fumarate; Aformoterol; CHEBI:63108; Atock; Foradil Aerolizer; Foradil formoterol, ((R*,R*)-(+-))-isomer; Oxis; formoterol fumarate, ((R*,R*)-(+-))-isomer |
In Vitro | In vitro activity: Formoterol is a potent airway smooth muscle relaxant with high efficacy, and very high affinity and selectivity for the beta 2-adrenoceptor. Formoterol appears to be retained in airway smooth muscle for extended periods since its relaxant effect on human airway smooth muscle is resistant to repeated washing and formoterol displays 'reassertion' of relaxation after washout of a beta-adrenoceptor antagonist. Formoterol has been demonstrated to potently inhibit these cells and processes in experimental test systems. Formoterol, like salbutamol and salmeterol, relaxes isolated preparations of guinea-pig trachea and human bronchus, and inhibits antigen-induced mediator release from human lung fragments in a concentration-related fashion. |
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In Vivo | Formoterol causes dose-related inhibition of histamine-induced bronchoconstriction in conscious guinea-pigs. Formoterol inhibits histamine-induced plasma protein extravasation (PPE) in guinea-pig lung, with significant inhibition being observed at 10 mg /mL and 100 mg /mL. Formoterol (100 mg /mL) inhibits PPE in guinea-pig lung for 2-4 hours, a duration of action intermediate between that previously obtained for salbutamol (1 hour) and salmeterol (> 6 hours). Formoterol inhibits neutrophil accumulation (lipopolysaccharide-induced) in guinea-pig lung but at doses greater than those required to inhibit granulocyte-independent PPE (histamine-induced). Formoterol (100 mg /mL) inhibits PAF-induced eosinophil accumulation in guinea-pig lung. |
Animal model | Guinea-pig |
Formulation & Dosage | 100 mg /mL |
References | Life Sci. 1993;52(26):2145-60; Eur J Pharmacol. 1994 Jan 14;251(2-3):127-35. |