Vitamin-D3-Cholecalciferol-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEVitaminD3Cat.No.:HY-15398CASNo.:67-97-0Synonyms:Cholecalciferol;Colecalciferol分?式:C??H??O分?量:384.64作?靶點:VD/VDR;EndogenousMetabolite;Bacterial作?通路:VitaminDRelated;MetabolicEnzyme/Protease;Anti-infection儲存?式:4°C,protectfromlight,storedundernitrogen*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?。溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(259.98mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.5998mL12.9992mL25.9983mL5mM0.5200mL2.5998mL5.1997mL10mM0.2600mL1.2999mL2.5998mL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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?.體內實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)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(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(5.41mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(5.41mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.41mM);ClearsolutionBIOLOGICALACTIVITY?物活性VitaminD3(Cholecalciferol;Colecalciferol)維?素D的天然存在形式，代謝激活后能誘導細胞分化和癌細胞增殖。IC50&TargetHumanEndogenousMetabolite體外研究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.體內研究Cholecalciferol(oralgavage;5mg/kg;7days)potentiatestheCCl4toxicityonlyintheliver,asindicatedbyplasmalevelsofALTandAST,biochemicalmarkersofhepaticdamage.Itsignificantlyincreasesrenalcalciumlevelsinmice,butrenalcalciumcontentdoesnotdiffersignificantlybetweenmice[3].2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:MaleddYmiceonCCl4toxicity[3]Dosage:5mg/kgAdministration:Oralgavage;5mg/kg;7daysResult:PotentiatedCCl4-inducedhepatotoxicityandenhancedmousemortality,withoutincreasingrenaltoxicityandgenerationofliverfibrosis.戶使?本產(chǎn)品發(fā)表的科研?獻?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