Laflunimus-HR325-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemELaflunimusCat.No.:HY-101813CASNo.:147076-36-6Synonyms:HR325分⼦式:C₁₅H₁₃F₃N₂O₂分⼦量:310.27作⽤靶点:DihydroorotateDehydrogenase;DNA/RNASynthesis;ProstaglandinReceptor作⽤通路:MetabolicEnzyme/Protease;CellCycle/DNADamage;GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(161.15mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2230mL16.1150mL32.2300mL5mM0.6446mL3.2230mL6.4460mL10mM0.3223mL1.6115mL3.2230mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.06mM);Clearsolution1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性Laflunimus(HR325)⼀种免疫抑制剂和Leflunomide活性代谢物A771726的类似物。Laflunimus⼀种⼝服的⼆氢硼酸脱氢酶(DHODH)抑制剂。Laflunimus抑制免疫球蛋⽩(Ig)分泌，抑制IgM和IgG分泌的IC50值分别为2.5和2μM。Laflunimus也前列腺素内过氧化物合酶(PGHS)-1和-2抑制剂。体外研究Igsecretionfrommousesplenocyteswasinducedbylipopolysaccharide(LPS)for5days.LaflunimusinhibitedthesecretionofIgMandIgGwithIC50valuesof2.5and2µM,respectively.AddingUridine(50µM)increasedthesevaluesto70and60µM,respectively.LaflunimusinhibitsLPS-inducedkappalight-chaincellsurfaceexpressionon70Z/3cells,apropertyalsoreversedbyuridine[1].Laflunimus(HR325)ismorepotentthanA771726asaninhibitorofPGHSinguineapigpolymorphonuclearleukocytes(IC50=415and4400nM,respectively)andonisolatedovinePGHS-1(IC50=64and742µM)andPGHS-2(IC50=100and2766µM)[2].体内研究HR325(50mg/kg;p.o.;days14-18afterbeinginjectedwithSRBC)inhibitsthesecondaryanti-sheepredbloodcell(SRBC)antibodyresponsewithID50valuesof38mg/kg[1].AnimalModel:MaleCD-1mice(20-24g)[1]Dosage:50mg/kgAdministration:Oral;days14-18afterbeinginjectedwithSRBCResult:Thelevelofcirculatinganti-SRBCIgGinthismodelwasinhibiteddoserelatedlybyorallyadministeredHR325.REFERENCES[1].ThomsonTA,etal.InvitroandinVivoinhibitionofimmunoglobulinsecretionbytheimmunosuppressivecompoundHR325isreversedbyexogenousuridine.ScandJImmunol.2002Jul;56(1):35-42.[2].CurnockAP,etal.PotenciesofleflunomideandHR325asinhibitorsofprostaglandinendoperoxideHsynthase-1and-2:comparisonwithnonsteroidalanti-inflammatorydrugs.JPharmacolExpTher.1997Jul;282(1):339-47.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplic