Andolast-CR-2039-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAndolastCat.No.:HY-106358ACASNo.:143330-46-5Synonyms:CR2039;Dizolast分?式:C??H??N?Na?O分?量:379.29作?靶點:Phosphodiesterase(PDE)作?通路:MetabolicEnzyme/Protease儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性數(shù)據(jù)體外實驗DMSO:12.5mg/mL(32.96mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6365mL13.1825mL26.3650mL5mM0.5273mL2.6365mL5.2730mL10mM0.2637mL1.3183mL2.6365mLBIOLOGICALACTIVITY?物活性Andolast(CR2039)?種抗過敏劑。Andolast可抑制cAMP-磷酸?酯酶，IC50值為50μM。Andolast可?于哮喘的研究。體內(nèi)研究Andolast(CR2039)(i.v.ori.m.)inhibitsratpassivecutaneousanaphylaxis(PCA)withanED50of0.1mg/kg[1].CR2039(10-100mg/kg;i.v.ori.m.)inhibitsthemicrovascularpermeabilitychangesinamodelofallergicconjunctivitisinsensitizedguinea-pigs[1].CR2039(0-1000μM;i.v.)inhibitsdosedependentlyguinea-piglungcAMP-phosphodiesterasewithanIC50valueof50μM[1].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:MaleHartleyguinea-pigs(300-500g)[1]Dosage:10-100mg/kgAdministration:I.M;I.V.Result:Showeddose-relatedsignificantprotectionagainstlgE-dependentbronchialanaphylaxisinducedbyaerosolizedantigeninanesthetizedguinea-pigs.Delayeddosedependentlytheonsetofbronchoconstrictioninducedbyaerosolizedantigen.REFERENCES[1].RevelL,ColomboS,FerrariF,FolcoG,RovatiLC,MakovecF.CR2039,anewbis-(1H-tetrazol-5-yl)phenylbenzamidederivativewithpotentialforthetopicaltreatmentofasthma.EurJPharmacol.1992;229(1):45-53.[2].CzuczwarSJ,GasiorM,KozickaM,PietrasiewiczT,TurskiWA,KleinrokZ.Apotentialanti-asthmaticdrug,CR2039,enhancestheanticonvulsiveactivityofsomeantiepilepticdrugsagainstpentetrazolinmice.EurNeuropsychopharmacol.1998;8(3):233-238.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400