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      Formoterol Hemifumarate
      Formoterol Hemifumarate

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V1134
      CAS #: 43229-80-7 Purity ≥98%

      Description: Formoterol Hemifumarate (CGP-25827A, NSC-299587, YM-08316; Eformoterol; Aformoterol; Atock; Foradil Aerolizer), the Hemifumarate salt of formoterol, is a selective and long-acting β2-adrenoceptor agonist with airway smooth muscle relaxing effects. It has been used in the management of asthma and chronic obstructive pulmonary disease (COPD with high efficacy, and very high affinity and selectivity for the beta 2-adrenoceptor.  

      References: Life Sci. 1993;52(26):2145-60; Eur J Pharmacol. 1994 Jan 14;251(2-3):127-35.

      Related CAS #: 43229-80-7 (fumarate)   73573-87-2 (free base)   183814-30-4 

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      Molecular Weight (MW)402.40 
      FormulaC19H24N2O4.1/2C4H4O4 
      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[[email protected]](CC1=CC=C(C=C1)OC)NC[[email protected]@H](C2=CC(=C(C=C2)O)NC=O)O.C[[email protected]](CC1=CC=C(C=C1)OC)NC[[email protected]@H](C2=CC(=C(C=C2)O)NC=O)O.C(=C/C(=O)O)\C(=O)O

      SynonymsEformoterol, 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


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      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.

      In VivoFormoterol 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 modelGuinea-pig
      Formulation & Dosage100 mg /mL
      References

      Life Sci. 1993;52(26):2145-60; Eur J Pharmacol. 1994 Jan 14;251(2-3):127-35. 

      These protocols are for reference only. InvivoChem does not independently validate these methods.

      Formoterol Hemifumarate

      Formoterol inhibits basal and thrombin-, but not PDGF-induced DNA synthesis in human PAVSM cells. Respir Res. 2012; 13(1): 109.
      		 

      Formoterol Hemifumarate

      Differential effects of formoterol on basal, thrombin- and PDGF-induced ERK1/2 phosphorylation in human PAVSM cells. Respir Res. 2012; 13(1): 109.
      		 

      Formoterol Hemifumarate

      Formoterol does not affect mTORC1 and mTORC2 activation by chronic hypoxia, thrombin and PDGF. Respir Res. 2012; 13(1): 109.

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