CRT0273750-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECRT0273750Cat.No.:HY-120797CASNo.:1979939-16-6分?式:C??H??ClF?N?O?分?量:502.92作?靶點(diǎn):Others作?通路:Others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:250mg/mL(497.10mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9884mL9.9419mL19.8839mL5mM0.3977mL1.9884mL3.9768mL10mM0.1988mL0.9942mL1.9884mL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(fù)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(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。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(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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:≥2.08mg/mL(4.14mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.14mM);ClearsolutionBIOLOGICALACTIVITY?物活性CRT0273750ATX抑制劑的先導(dǎo)化合物，并調(diào)節(jié)?漿中LPA?平。CRT0273750可?于ATX/LPA依賴性癌癥模型[1]。IC50&TargetIC50:0.014μM(plasmaCRA)體外研究CRT0273750showshighpotencyinboththebiochemical(IC50=0.01μM)andplasmacholinereleaseassay(IC50=0.014μM)[1].CRT0273750isalsoshowntoinhibitthemigrationof4T1cellswithanEC50of0.025μM[1].體內(nèi)研究CRT0273750(1mg/kg;i.v.)hasamoderatebloodclearance,withvalueof41mL/min/kg[1].CRT0273750(10mg/kg;oraladministration)treatmentshowstheCmax,AUCandt1/2valuesof3.8μM,3.2μM.hand1.4h,respectively[1].CRT0273750(10,30and100mg/kg;oraladministration)showsaproportionalincrease[1].AnimalModel:CD-1mice[1]Dosage:1mg/kgAdministration:I.v.Result:Hadamoderatebloodclearance.AnimalModel:Balb-cnu/numice[1]Dosage:10,30and100mg/kgAdministration:Oraladministration(PharmacokineticAnalysis)Result:TheCmaxswere3.8,10.9and18.1μM,respectively.TheAUCswere3.2,15.2and59.3μM.h,respectively.Thet1/2swere1.4,0.9and1.3h,respectively.REFERENCES[1].ShahP,etal.Discoveryofpotentinhibitorsofthelysophospholipaseautotaxin.BioorgMedChemLett.2016;26(22):5403-5410.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchus