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Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVitaminD3Cat.No.:HY-15398CASNo.:67-97-0Synonyms:Cholecalciferol;Colecalciferol分⼦式:C₂₇H₄₄O分⼦量:384.64作⽤靶点:VD/VDR;EndogenousMetabolite;Bacterial作⽤通路:VitaminDRelated;MetabolicEnzyme/Protease;Anti-infection储存⽅式:4°C,protectfromlight,storedundernitrogen*该产品在溶液状态不稳定,建议您现⽤现配,即刻使⽤。溶解性数据体外实验DMSO:100mg/mL(259.98mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5998mL12.9992mL25.9983mL5mM0.5200mL2.5998mL5.1997mL10mM0.2600mL1.2999mL2.5998mL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;该产品在溶液状态不稳定,建议您现⽤现配,即刻使⽤.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%salineSolubility:≥2.08mg/mL(5.41mM);Clearsolution2.请依序添加每种溶剂:10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(5.41mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE3.请依序添加每种溶剂:10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.41mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性VitaminD3(Cholecalciferol;Colecalciferol)维⽣素D的天然存在形式,代谢激活后能诱导细胞分化和癌细胞增殖。IC50&TargetHumanEndogenousMetabolite体外研究VitaminD3isaninactivevitaminDmoleculeinvivo.VitaminD3undergoestwohydroxylationprocessestoactivateit.VitaminD3isfirsthydroxylatedinthelivertoformthecirculatingprohormone25-hydroxyvitaminD3[25(OH)D3]bytheenzyme25-hydroxylase(CYP27A1)andprobablyalsobyotherenzymes(e.g.,CYP2R1)[1].Thesecondhydroxylationoccursinthekidneysviatheenzyme1-alpha-hydroxylase,yielding1,25-dihydroxycholecalciferol(calcitriol),whichisthebiologicallyactiveformofvitaminD[1].VitaminD3(2-10μM;24-48hours)exhibitsanti-proliferativeeffectsinadose-andtime-dependentmanner.Maximalreductionofviabilityposttreatmentof62%(IK),52%(RL-95-2),and55%(Hec-1A)occurrsby72hoftreatmentwith10μMVitaminD3.but24-hourexposurelackssignificantreductioninviablecells[2].Cholecalciferol(10μM;24-48hours)showsmarkedincreasesinnuclearVDRstainingandproduceslocalVDRactivationinIKcells[1].CellViabilityAssay[2]CellLine:ECcelllinesfromEEC,Ishikawa3-H-12(IK),RL-95/2,andHEC-1-AcellsConcentration:2-10μMIncubationTime:24-72hoursResult:ReducedviabilityinresponsetoVD3inadose-andtime-dependentmanner.IndicatedthattheconversionofVD3to25(OH)Disanessentialstepforthereducedcellviabilityeffect.CellViabilityAssay[2]CellLine:ECcelllinesfromEEC,Ishikawa3-H-12(IK)cellsConcentration:10μMIncubationTime:24-48hoursResult:ImprovednuclearVDRcontentinIKcells.体内研究Cholecalciferol(oralgavage;5mg/kg;7days)potentiatestheCCl4toxicityonlyintheliver,asindicatedbyplasmalevelsofALTandAST,biochemicalmarkersofhepaticdamage.Itsignificantlyincreasesrenalcalciumlevelsinmice,butrenalcalciumcontentdoesnotdiffersignificantlybetweenmice[3].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:MaleddYmiceonCCl4toxicity[3]Dosage:5mg/kgAdministration:Oralgavage;5mg/kg;7daysResult:PotentiatedCCl4-inducedhepatotoxicityandenhancedmousemortality,withoutincreasingrenaltoxicityandgenerationofliverfibrosis.户使⽤本产品发表的科研⽂献•IntJOralSci.2022Aug1;14(1):39.•NatChemBiol.2022Aug18.•SmallMethods.16December2021.•ProcNatlAcadSciUSA.2022Apr12;119(15):e2117004119.•MolNutrFoodRes.2021Dec11;e2100952.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].NazikAl-Hashimi,etal.Cholecalciferol[2].LauraBergadà,etal.RoleoflocalbioactivationofvitaminDbyCYP27A1andCYP2R1inthecontrolofcellgrowthinnormalendometriumandendometrialcarcinoma.LabInvest.2014Jun;94(6):608-22[3].HirokiYoshioka,etal.VitaminD3-inducedhypercalcemiaincreasescarbontetrachloride-inducedhepatotoxicitythroughelevatedoxidativestressinmice.PLoSOne.2017Apr27;12(4):e0176524.M

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