Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECalpeptinCat.No.:HY-100223CASNo.:117591-20-5分?式:C??H??N?O?分?量:362.46作?靶點:Cathepsin;Proteasome;Apoptosis作?通路:MetabolicEnzyme/Protease;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(275.89mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.7589mL13.7946mL27.5893mL5mM0.5518mL2.7589mL5.5179mL10mM0.2759mL1.3795mL2.7589mL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；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)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(nèi)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:≥2.5mg/mL(6.90mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.90mM);ClearsolutionBIOLOGICALACTIVITY?物活性Calpeptin?種有效的、具有細胞穿透性的calpain抑制劑，其對???板CalpainI的ID50值為40nM[1]。Calpeptin也cathepsinK的抑制劑[2]。IC50&TargetID50:40nM(CalpainIinhumanplatelets)[1].CthepsinK[2]體外研究Calpeptin(0-100nM,24hours)treatmentsuppressestheproliferationofbothWI38VA13andIMR90cellsinadose-dependentmanner.Calpeptin(1000pg/ml,24hours)inhibitsIL-6-inducedcellproliferationoflungfibroblasts[3].CellProliferationAssay[3]CellLine:WI38VA13andIMR90cellsConcentration:0-100nMIncubationTime:24hoursResult:Suppressedtheproliferationinadose-dependentmanner.體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻?ACSCentSci.February2,2022.?JNanobiotechnology.2022Mar28;20(1):165.?AntioxidRedoxSignal.2022Nov4.?JCellMolMed.2020Aug;24(16):9287-9299.?ChemBiolInteract.2022Jul1;361:109967.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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