Calpeptin-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemECalpeptinCat.No.:HY-100223CASNo.:117591-20-5分?式:C??H??N?O?分?量:362.46作?靶點(diǎn):Cathepsin;Proteasome;Apoptosis作?通路:MetabolicEnzyme/Protease;Apoptosis儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(275.89mM;Needultrasonic)掃描?維碼，H2O:<0.1mg/mL(insoluble)運(yùn)?溶解?案計(jì)算器獲得適合您實(shí)驗(yàn)體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.7589mL13.7946mL27.5893mL5mM0.5518mL2.7589mL5.5179mL10mM0.2759mL1.3795mL2.7589mL請(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶1.請(qǐng)依序添加每種溶劑：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.5mg/mL(6.90mM);Clearsolution此?案可獲得≥2.5mg/mL(6.90mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲(chǔ)備液加到400μLPEG300中，混合均勻；向上述體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。1/3www.MedChemEwww.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥2.5mg/mL(6.90mM);Clearsolution此?案可獲得≥2.5mg/mL(6.90mM，飽和度未知)的澄溶液，此?案不適?于實(shí)驗(yàn)周期在半個(gè)?以上的實(shí)驗(yàn)。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲(chǔ)備液加到900μL??油中，混合均勻。BIOLOGICALACTIVITY?物活性Calpeptin?種有效的、具有細(xì)胞穿透性的calpain抑制劑，其對(duì)???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(xiàn)?JCellMolMed.2020Aug;24(16):9287-9299.?RSCAdv.2019,2019,9,25107-25118.?IntJMedSci.2021;18(8):1746-1752.2/3www.MedChemEwww.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.McePdfHeight關(guān)注MCE中國(guó)公眾號(hào)，

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