Reldesemtiv-CK-2127107-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEReldesemtivCat.No.:HY-109121CASNo.:1345410-31-2Synonyms:CK-2127107分⼦式:C₁₉H₁₈F₂N₆O分⼦量:384.38作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(650.40mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.6016mL13.0080mL26.0159mL5mM0.5203mL2.6016mL5.2032mL10mM0.2602mL1.3008mL2.6016mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(5.41mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.41mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.41mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Reldesemtiv(CK-2127107)⼀种选择性的，⼝服活性的下⼀代快速⾻骼肌肌钙蛋⽩(fastskeletalmuscletroponin)激活剂(FSTA)。Reldesemtiv选择性激活快速⾻骼肌原纤维，EC50为3.4μM。Reldesemtiv可提⾼⼼⼒衰竭模型的运动表现。体外研究Reldesemtivselectivelybindstoandsensitizesthefastskeletaltroponincomplextocalcium[1].体内研究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