Radioprotectin-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERadioprotectin-1Cat.No.:HY-114380CASNo.:1622006-09-0分⼦式:C₂₃H₁₉ClN₂O₆S分⼦量:486.92作⽤靶点:LPLReceptor作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(256.72mM;Needultrasonic)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0537mL10.2686mL20.5373mL5mM0.4107mL2.0537mL4.1075mL10mM0.2054mL1.0269mL2.0537mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(4.27mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.27mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.27mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Radioprotectin-1⼀种⾼效特异性的溶⾎磷脂酸受体2(LPA2)激动剂，EC50值为25nM(⿏LPA2亚型)[1]。IC50&TargetEC50:25nM(murineLPA2subtype)[1]体外研究Radioprotectin-1isapotentagonistofLPA2withanEC50of5pMandfunctionsasafullagonistatthehumanorthologofLPA2[1].Radioprotectin-1(0-3μM;15minutes)effectivelyreducesapoptosisinducedbyγ-irradiationandtheradiomimeticdrugAdriamycinincellsthatexpressedLPA2eitherendogenouslyoraftertransfection[1].CellViabilityAssay[1]CellLine:MEFcells,IEC-6cellsConcentration:0μM,0.1μM,0.3μM,1.0μM,3μMIncubationTime:15minutesResult:Protectedcellsfromapoptosisbyγ-irradiation-andtheradiomimeticchemotherapeuticAdiamycin.体内研究Radioprotectin-1isahigh-potencyspecificagonistofthemurineLPA2GPCR[1].Radioprotectin-1(0.1mg/kg,0.3mg/kg;s.c.;every12hours;for3days)decreasesthemortalityofC57BL/6miceinmodelsofthehematopoieticacuteradiationsyndromes(HE-ARS)andgastrointestinalacuteradiationsyndromes(GI-ARS)[1].Radioprotectin-1exertsitsradioprotectiveandradiomitigativeactionthroughspecificactivationoftheupregulatedLPA2GPCRinLgr5+stemcells[1].AnimalModel:8-10weeksoldC57BL/6femalemicebearingtotalbodyirradiation(TBI)[1]Dosage:0.1mg/kg,0.3mg/kgAdministration:Subcutaneousinjection;every12hours;for3daysResult:DecreasedmortalityofC57BL/6miceinmodelsoftheHE-ARSandtheGI-ARS.REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].KuoB,etal.TheLPA2receptoragonistRadioprotectin-1sparesLgr5-positiveintestinalstemcellsfromradiationinjuryinmurineenteroids.CellSignal.2018Nov;51:23-33.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformed