Calhex-231-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECalhex231hydrochlorideCat.No.:HY-103320ACASNo.:2387505-78-2分⼦式:C₂₅H₂₈Cl₂N₂O分⼦量:443.41作⽤靶点:CaSR作⽤通路:GPCR/GProtein储存⽅式:-20°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:33.33mg/mL(75.17mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2552mL11.2762mL22.5525mL5mM0.4510mL2.2552mL4.5105mL10mM0.2255mL1.1276mL2.2552mL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(sealedstorage,awayfrommoisture)。-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%salineSolubility:2.5mg/mL(5.64mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.64mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性Calhex231hydrochloride⼀种通过负变构调节来抑制CaSR的。Calhex231hydrochloride在HEK293细胞中阻断Ca2+诱导的肌醇磷酸酯的积累，IC50为0.39μM。Calhex231hydrochloride可⽤于糖尿病性⼼肌病(DCM)的研究。IC50&TargetCaSR[1]IC50:0.39μM(Inositolphosphate)[2]体外研究Calhex231treatmentsignificantlydecreasestheproliferationofcardiacfibroblasts[1].Calhex231treatmentsignificantlydownregulatestheCaSR,α-SMA,Col-I/III,MMP2/9expresses.Calhex231alleviateshighglucose-inducedmyocardialfibrosisincardiacfibroblasts[1].Calhex231couldinhibitItch(atrophin-1interactingprotein4)-ubiquitinproteasomeandTGF-β1/Smadspathways,andthendepresstheproliferationofcardiacfibroblasts,alongwiththereductiondepositionofcollagen,alleviateglucose-inducedmyocardialfibrosis[1].CellProliferationAssay[1]CellLine:Primaryneonatalratcardiacfibroblasts(CFs)Concentration:3µMIncubationTime:24hoursResult:Significantlydecreasedtheproliferationofcardiacfibroblasts.WesternBlotAnalysis[1]CellLine:Primaryneonatalratcardiacfibroblasts(CFs)Concentration:3µMIncubationTime:48hoursResult:TheexpressionofCaSR,α-SMA,Col-I/III,MMP2/9weresignificantlydownregulated.体内研究Calhex231(4.07mg/kg(10µmol/kg);intraperitonealinjection;daily;for12weeks;maleWistarrats)treatmentamelioratesdiabeticmyocardialfibrosisintype1diabeticmodel(T1D)rats[1].AnimalModel:MaleWistarrats(8weeksold)injectedwithStreptozotocin[1]Dosage:4.07mg/kg(10µmol/kg)Administration:Intraperitonealinjection;daily;for12weeksResult:AmeliorateddiabeticmyocardialfibrosisinT1Drats.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE户使⽤本产品发表的科研⽂献•FrontPharmacol.2022Feb23;13:816133.•FrontPharmacol.23February2022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].YuanH,etal.Calhex231AlleviatesHighGlucose-InducedMyocardialFibrosisviaInhibitingItch-UbiquitinProteasomePathwayinVitro.BiolPharmBull.2019Aug1;42(8):1337-1344.[2].PetrelC1,etal.ModelingandmutagenesisofthebindingsiteofCalhex231,anovelnegativeallostericmodulatoroftheextracellularCa(2+)-sensingreceptor.JBiolChem.2003Dec5;278(49):49487-94.McePdfHeightCaution:Producthasnotbe