Mefentrifluconazole-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEMefentrifluconazoleCat.No.:HY-136063CASNo.:1417782-03-6分?式:C??H??ClF?N?O?分?量:397.78作?靶點(diǎn):Fungal;CytochromeP450作?通路:Anti-infection;MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(251.40mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.5140mL12.5698mL25.1395mL5mM0.5028mL2.5140mL5.0279mL10mM0.2514mL1.2570mL2.5140mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥6.25mg/mL(15.71mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥6.25mg/mL(15.71mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥6.25mg/mL(15.71mM);Clearsolution1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性Mefentrifluconazole?種新型的唑類衍?物，?譜抗真(antifungalagent)劑。Mefentrifluconazole是具有強(qiáng)效選擇性和?服活性真CYP51的抑制劑(Kd=0.5nM)，但對?類芳?化酶(IC50=0.92μM)的抑制活性較?。IC50&TargetCYP51A0.5nM(Kd)體內(nèi)研究Mefentrifluconazoleundergoesextensivetoxicitytesting,includingafullprogramofreproductivetoxicitystudies.Longtermrepeateddosetoxicityand/orcarcinogenicitystudieshavebeenconductedinrats,mice,anddogs.Ineachspecies,thehighestdoselevelinvestigatedgivesrisetosystemictoxicity[1].IntheacuteandrepeatdosetoxicitystudiesperformedwithMefentrifluconazole.Asingle-doseadministrationtoratstheLD50is>2000?mg/kgbwtbytheoralroute,>5000?mg/kgbwtbythedermalroute,and>5.314?mg/Lbyinhalationasadustaerosol.Mefentrifluconazoleisnotaskinoraneyeirritant,norisitaphototoxicantinvitro[1].Intheacuteneurotoxicitystudyinrats,Mefentrifluconazole(oraladministration;2000?mg/kgbwt;singledose)givesrisetoreducebodyweightgainandtransientneurobehavioraleffectsonlyonthedayoftreatment(unsteadygait,reducedmotoractivity,reducesgripstrengthoftheforelimbsandincreaseddistancebetweenthehindlimbsinthelandingfoot-splaytest)[1].Intherepeated-dosetoxicitystudies,theliveristhetargetorganineachofthethreespeciesinvestigated.Athigherdoselevelsintherat(oraldiets;383/334mg/kg/bwt/d(4000ppm))andtheC57BL/6JRjmouse(61mg/kgbwt/d(300ppm)),reducesbodyweightgainandfoodconsumption,altersclinicalchemistryparameters,increasesliverweightandisaccompaniedbylivercellhypertrophy,and/orlivercellnecrosis.Atlowdoses,increasesliverweightisnotassociatedwithanyhistopathologicalalterationsandisconsideredtobeanadaptivechangetotreatment[1].REFERENCES[1].TeshSA,etal.Innovativeselectionapproachforanew