Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDihydromunduletoneCat.No.:HY-101483CASNo.:674786-20-0Synonyms:DHM分?式:C??H??O?分?量:424.49作?靶點:Others作?通路:Others儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:250mg/mL(588.94mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3558mL11.7788mL23.5577mL5mM0.4712mL2.3558mL4.7115mL10mM0.2356mL1.1779mL2.3558mL請根據產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?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，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沉淀、析出現象，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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.90mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.90mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.90mM);ClearsolutionBIOLOGICALACTIVITY?物活性Dihydromunduletone(DHM)類胡蘿?素衍?物，?種選擇性，有效的粘附G蛋?偶聯受體(aGPCR)(GPR56andGPR114/ADGRG5)拮抗劑，對GPR56的IC50值為20.9μM，但不抑制GPR110或A類GPCR。IC50&TargetIC50:20.9μM(GPR56)[1];GPR114[1]體外研究Assaysareinitiatedbytheadditionof[35S]GTPγS,andtheratesofaGPCR-stimulatedGproteinactivation([35S]GTPγSbindingtoGα)aremeasuredwithorwithouttheinfluenceofaddedcompounds.Dihydromunduletone(DHM)inhibitsthekineticsofGPR567TM-stimulatedG13GTPγSbindingtovaryingdegrees.DihydromunduletoneisthebestinhibitorycompoundandreducedtherateatwhichGPR567TMactivatedG13>75%(from0.18to0.04minute?1)[1].AtaconcentrationofDihydromunduletone(DHM)thatmaximallyinhibitsGPR56(50μM),therateofGPR1147TM-stimulatedGsactivityisalsoinhibiteddramatically.WhenDihydromunduletone(50μM)isappliedtotheGPR1107TM,itfailstoinhibitGPR110stimulationofGqGTPγSbinding[1].CellstransfectedwithGPR56A386M7TMareincubatedwithincreasingconcentrationsofDihydromunduletone.P7peptideagonistisadded,andSRE-luciferaseactivityismeasured.DihydromunduletoneinhibitstheP7peptide-inducedluciferaseactivityinaconcentration-dependentmanner.Cellsarealsotreatedwithafixedconcentrationof3μMDihydromunduletoneandthenstimulatedwithanincreasingconcentrationofP7peptideagonist.DihydromunduletonetreatmentbluntsP7peptideactivationateachconcentration.Inconclusion,Dihydromunduletoneantagonizessynthetic-peptideagonistandtethered-peptideagonist-mediatedaGPCRactivationinisolatedmembranesandHEK293Tcell-basedassays,butitdoesnotinhibitbasalreceptorsignaling[1].REFERENCES[1].HannahM.Stoveken,etal.DihydromunduletoneIsaSmall-MoleculeSelectiveAdhesionGProtein–CoupledReceptorAntagonist.MolPharmacol.2016Sep;90(3):214–224.McePdfHeightCaution:Producthasnotbeenfullyvalidated