LDH-IN-1-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELDH-IN-1Cat.No.:HY-111108CASNo.:1964515-43-2分?式:C??H??N?O?S?分?量:570.68作?靶點:LactateDehydrogenase作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:52mg/mL(91.12mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.7523mL8.7615mL17.5230mL5mM0.3505mL1.7523mL3.5046mL10mM0.1752mL0.8761mL1.7523mL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；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.17mg/mL(3.80mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.17mg/mL(3.80mM);ClearsolutionBIOLOGICALACTIVITY?物活性LDH-IN-1?種新的于吡唑的?乳酸脫氫酶(LDH)抑制劑，對于LDHA和LDHB的IC50值分別為32和27nM。IC50&TargetIC50:32nM(LDHA),27nM(LDHB)[1]體外研究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].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?CellRep.2022Jun21;39(12):110986.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].RaiG,etal.DiscoveryandOptimizationofPotent,Cell-ActivePyrazole-BasedInhibitorsofLactateDehydrogenase(LDH).JMedChem.2017Nov22;60(22):9184-9204.McePdfHeightCaution: