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

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELDH-IN-1Cat.No.:HY-111108CASNo.:1964515-43-2分⼦式:C₃₀H₂₆N₄O₄S₂分⼦量:570.68作⽤靶点:LactateDehydrogenase作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:52mg/mL(91.12mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7523mL8.7615mL17.5230mL5mM0.3505mL1.7523mL3.5046mL10mM0.1752mL0.8761mL1.7523mL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:≥2.17mg/mL(3.80mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.17mg/mL(3.80mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性LDH-IN-1⼀种新的于吡唑的⼈乳酸脱氢酶(LDH)抑制剂，对于LDHA和LDHB的IC50值分别为32和27nM。IC50&TargetIC50:32nM(LDHA),27nM(LDHB)[1]体外研究LDH-IN-1exhibitslownMinhibitionofbothLDHAandLDHB(IC50=32,27nM,respectively),submicromolarinhibitionoflactateproduction,andinhibitionoflactateinMiaPaCa2pancreaticcancerandA673sarcomacells(IC50=0.517,0.854μM,respectively).LDH-IN-1inhibitsthegrowthofMiaPaCa2pancreaticcancerandA673sarcomacellswithIC50sof2.23and1.21μM).Dose−responsetreatmentofMiaPaCa-2cellswithLDH-IN-1showseffectsoncellularproliferationatconcentrationsaslowas250nMandwithnearlycompletearrestofcellgrowthat20μM[1].体内研究LDH-IN-1showsclearancevaluesthatfarexceedhepaticbloodflow(HBF)inmousespecies(90mL/min/kg),withinvivoclearancesof227mL/min/kg[1].PROTOCOLCellAssay[1]A673andMiaPaCa-2cellsA673andMiaPaCa-2cellsareculturedandplatedin1536-wellwhitesolidtissuecultureplates.A1536-wellpintooldispenseroutfittedwith20nLpinsisusedtotransfer23nLofLDH-IN-1inDMSOtothe1536-wellassayplates.Aftera48hincubationat37°C,2.5μLofCellTiter-GloisdispensedintoeachwellusingaBioRAPTRFRDdispenser.Platesareincubatedatroomtemperaturefor10min,transferredtoaViewLuxmicroplateimager,andtheATP-coupledluminescenceismeasuredusinga1sexposure[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[1]Administration[1]MaleCD1miceapproximately6−8weeksofageandaweightofapproximately20−30g,aredosedwithLDH-IN-1at2mg/kg(iv)and50mg/kg(po).Eachcohorthadthreemice,andplasmaiscollectedat5min,15min,30min,1h,2h,4h,8h,12h,and24hpostdoseforivand15min30min,1h,2h,4h,8h,12h,and24hforpo.Approximately0.025mLofbloodiscollectedviathedorsalmetatarsalveinateachtimepoint.Bloodsamplesarethentransferredintoplasticmicrocentrifugetubescontainingheparin−Naasanticoagulant.Samplesarethencentrifugedat4000gfor5minat4°Ctoobtainplasma.Plasmasamplesarethenstoredinpolypropylenetubes,quicklyfrozen,andkeptat−75°CuntilanalyzedbyLC/MS/MS[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•CellRep.2022Jun21;39(12):110986.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].RaiG,etal.DiscoveryandOptimizationofPotent,Cell-ActivePyrazole-BasedInhibitorsofLactateDehydrogenase(LDH).JMedChem.2017Nov22;60(22):9184-9204.McePdfHeightCaution: