Reldesemtiv-CK-2127107-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEReldesemtivCat.No.:HY-109121CASNo.:1345410-31-2Synonyms:CK-2127107分?式:C??H??F?N?O分?量:384.38作?靶點(diǎn):Others作?通路:Others儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:250mg/mL(650.40mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6016mL13.0080mL26.0159mL5mM0.5203mL2.6016mL5.2032mL10mM0.2602mL1.3008mL2.6016mL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(fù)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?jiān)?個?內(nèi)使?，-20°C儲存時，請?jiān)?個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?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(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥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);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.41mM);ClearsolutionBIOLOGICALACTIVITY?物活性Reldesemtiv(CK-2127107)?種選擇性的，?服活性的下?代快速?骼肌肌鈣蛋?(fastskeletalmuscletroponin)激活劑(FSTA)。Reldesemtiv選擇性激活快速?骼肌原纖維，EC50為3.4μM。Reldesemtiv可提???衰竭模型的運(yùn)動表現(xiàn)。體外研究Reldesemtivselectivelybindstoandsensitizesthefastskeletaltroponincomplextocalcium[1].體內(nèi)研究Reldesemtiv(10mg/kg;p.o.)significantlyimprovesrotarodperformanceinexercise-intolerantLAD-HFrats[1].Reldesemtiv(10mg/kg;i.v.)increasesCa2+sensitivityinfastskeletalmusclefibersandincreasesmuscleforceinresponsetosubmaximalstimulationfrequenciesinLAD-HFrats[1].ReldesemtivincreasessarcomericCa2+sensitivityinskinnedLAD-HFskeletalfibers[1].AnimalModel:FemaleSprague-Dawleyrats(Shamandleftanteriordescendingcoronaryartery(LAD)heartfailure(LAD-HF))[1]Dosage:10mg/kgAdministration:p.o.Result:Increasedperformancetimebyapproximately150%inLAD-HFrats(116±22versus283±47seconds).REFERENCES[1].HweeDT,etal.Thesmall-moleculefastskeletaltroponinactivator,CK-2127107,improvesexercisetoleranceinaratmodelofheartfailure.JPharmacolExpTher.2015Apr;353(1):159-68.[2].AndrewsJA,etal.CK-2127107amplifiesskeletalmuscleresponsetonerveactivationinhumans.MuscleNerve.2018May;57(5):729-734.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forr