Calpeptin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECalpeptinCat.No.:HY-100223CASNo.:117591-20-5分⼦式:C₂₀H₃₀N₂O₄分⼦量:362.46作⽤靶点:Cathepsin;Proteasome;Apoptosis作⽤通路:MetabolicEnzyme/Protease;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(275.89mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7589mL13.7946mL27.5893mL5mM0.5518mL2.7589mL5.5179mL10mM0.2759mL1.3795mL2.7589mL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%salineSolubility:≥2.5mg/mL(6.90mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.90mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Calpeptin⼀种有效的、具有细胞穿透性的calpain抑制剂，其对⼈⾎⼩板CalpainI的ID50值为40nM[1]。Calpeptin也cathepsinK的抑制剂[2]。IC50&TargetID50:40nM(CalpainIinhumanplatelets)[1].CthepsinK[2]体外研究Calpeptin(0-100nM,24hours)treatmentsuppressestheproliferationofbothWI38VA13andIMR90cellsinadose-dependentmanner.Calpeptin(1000pg/ml,24hours)inhibitsIL-6-inducedcellproliferationoflungfibroblasts[3].CellProliferationAssay[3]CellLine:WI38VA13andIMR90cellsConcentration:0-100nMIncubationTime:24hoursResult:Suppressedtheproliferationinadose-dependentmanner.体内研究CalpeptinwithBleo(0.04mg/mouse,i.p.,3timesweekly,28days)administrationsignificantlyinhibitsthecollagendepositionandincreasesofcalpainactivityintheNSC-125066treatedmouselungtissues[3].AnimalModel:C57BL/6femalemice(Eight-week-old)[3].Dosage:0.04mg/mouse.Administration:Intraperitoneallythreetimesweeklyfor28days(togetherwithBleo).Result:InhibitedthecollagendepositionandincreaseofcalpainactivityintheNSC-125066treatedmouselungtissues.户使⽤本产品发表的科研⽂献•ACSCentSci.February2,2022.•JNanobiotechnology.2022Mar28;20(1):165.•AntioxidRedoxSignal.2022Nov4.•JCellMolMed.2020Aug;24(16):9287-9299.•ChemBiolInteract.2022Jul1;361:109967.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].TsujinakaT,etal.Synthesisofanewcellpenetratingcalpaininhibitor(calpeptin).BiochemBiophysResCommun.1988Jun30;153(3):1201-8.[2].CatalanoJG,etal.Designofsmallmoleculeketoamide-basedinhibitorsofcathepsinK.BioorgMedChemLett.2004Feb9;14(3):719-22.[3].TabataC,etal.Thecalpaininhibitorcalpeptinpreventspulmonaryfibrosisinmice.ClinExpImmunol.2010Dec;162(3):560-7.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor