FD-IN-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFD-IN-1Cat.No.:HY-128570CASNo.:1646682-14-5分⼦式:C₂₃H₂₃NO₄分⼦量:377.43作⽤靶点:ComplementSystem作⽤通路:Immunology/Inflammation储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:62.5mg/mL(165.59mM;ultrasonicandwarmingandheatto80°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.6495mL13.2475mL26.4950mL5mM0.5299mL2.6495mL5.2990mL10mM0.2649mL1.3247mL2.6495mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.51mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.51mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.51mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性FD-IN-1(Compound12)⼀种有效的，具有⼝服活性的补体因⼦D(FD)抑制剂，IC50为12nM。补体因⼦D⼀种⾼特异性的S1丝氨酸蛋⽩酶，在先天免疫系统的替代补体途径中起重作⽤。FD-IN-1还抑制因⼦XIa(FXIa)和类胰蛋⽩酶β2，IC50分别为7.7和6.5μM[1]。体外研究FD-IN-1(Compound12)exhibitsfunctionalinhibitionofAPactivation(IC50=0.26μM)invitroinamembraneattackcomplex(MAC)depositionassayusing50%humanwholeblood(WB)[1].体内研究FD-IN-1(Compound12)demonstratessystemicsuppressionofAPactivationinalipopolysaccharide-inducedalternativecomplementpathway(AP)activationmodelaswellaslocalocularsuppressioninintravitrealinjection-inducedAPactivationmodelinmiceexpressinghumanFD[1].FD-IN-1(Compound12)exhibitshighoralbioavailability(C57BL6mice83%,Beagledogs70%)followingoraladministration(miceanddogs10mg/kg)[1].FD-IN-1(Compound12)exhibitsterminaleliminationhalf-lives(C57BL6mice1.6handBeagledogs3.8h)followingintravenousadministration(miceanddogs1mg/kg)[1].AnimalModel:HumanFDknock-inmice[1]Dosage:3and10mg/kgAdministration:OralgavageResult:TheAPpathwaywasfullyinhibitedforupto10hatthe10mg/kgdose.REFERENCES[1].KarkiRG,etal.Design,Synthesis,andPreclinicalCharacterizationofSelectiveFactorDInhibitorsTargetingtheAlternativeComplementPathway.JMedChem.2019May9;62(9):4656-4668.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.