Fluorometholone-acetate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEFluorometholoneacetateCat.No.:HY-B1471CASNo.:3801-06-7分⼦式:C₂₄H₃₁FO₅分⼦量:418.5作⽤靶点:CarbonicAnhydrase作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(597.37mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3895mL11.9474mL23.8949mL5mM0.4779mL2.3895mL4.7790mL10mM0.2389mL1.1947mL2.3895mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存⽅式和期限。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.97mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.97mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.97mM);Clearsolution1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性Fluorometholoneacetate⼀种合成的糖⽪质激素⽪质类醇和⽪质类醇酯。Fluorometholoneacetate有效抑制碳酸酐酶(CA)对hCA-I和hCA-II的IC50分别为2.18μM和17.5μM。Fluorometholoneacetate具有抗炎作⽤，可⽤于外部眼部炎症的研究。IC50&TargetIC50:2.18μM(humancarbonicanhydrase(hCA)-I)and17.5μM(hCA-II)[2]Ki:1.044μM(hCA-I)and9.98μM(hCA-II)[2]体外研究ForFluorometholoneacetate,aKivaluefromLineweaver-Burkplotsisobtainedas1.044μM(noncompetitive)forhCA-Iand9.98μM(non-competitive)forhCA-II[2].体内研究Hourlytopicaladministrationof0.1%Fluorometholoneacetateophthalmicsuspensionproduced,ontheaverage,a47%reductioninthepolymorphonuclearleukocytesinvadingthecorneaduringanexperimentallyinducedinflammatorykeratitisinNewZealandalbinorabbits(1.5-2.0kg).Fluorometholoneacetate(0.1%)formulatedasahigh-viscositycarbomergelandappliedatthree-hourintervalsreducedinvadingleukocytesinthecorneaanaverageof48%,aneffectnotsignificantlydifferentfromhourlyadministrationofthesuspension[1].REFERENCES[1].AKupferman,etal.Fluorometholoneacetate.Anewophthalmicderivativeoffluorometholone.ArchOphthalmol.1982Apr;100(4):640-1.[2].ZuhalAlım,etal.SomeAnti-InflammatoryAgentsInhibitEsteraseActivitiesofHumanCarbonicAnhydraseIsoformsIandII:AnInVitroStudy.ChemBiolDrugDes.2015Oct;86(4):857-63.[3].HMLeibowitz,etal.Fluorometholoneacetate:clinicalevaluationinthetreatmentofexternalocularinflammation.AnnOphthalmol.1984Dec;16(12):1110-5.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicati