NKH477-Colforsin-dapropate-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENKH477Cat.No.:HY-103193CASNo.:138605-00-2Synonyms:Colforsindapropatehydrochloride分⼦式:C₂₇H₄₄ClNO₈分⼦量:546.09作⽤靶点:AdenylateCyclase作⽤通路:GPCR/GProtein储存⽅式:-20°C,storedundernitrogen,awayfrommoisture*该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。溶解性数据体外实验DMSO:125mg/mL(228.90mM;Needultrasonic)H2O:20mg/mL(36.62mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8312mL9.1560mL18.3120mL5mM0.3662mL1.8312mL3.6624mL10mM0.1831mL0.9156mL1.8312mL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；该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤.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:≥2.08mg/mL(3.81mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(3.81mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.81mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性NKH477(Colforsindapropatehydrochloride)直接激活腺苷酸环化酶(adenylatecyclase)的催化单元并增加细胞内cAMP。NKH477⼀种⽑喉素衍⽣物，主通过对舒张性⼼脏功能的有益作⽤来改⼼⼒衰竭。NKH477在体内抗增殖作⽤，可以抑制⼤⿏原位肺同种异体移植物的急性排斥。IC50&TargetAdenylateCyclase[1]体内研究NKH477(Colforsindapropatehydrochloride)(orally;1-3mg/kg/day;days3and5)prolongedlungallograftsurvivalinadosedependentmanner[1].AnimalModel:Specific-pathogen-freeinbredmaleLewisrats(LEW)weighing250to280g[1]Dosage:1,2or3mg/kg/dayAdministration:Orally;daily;Days3and5Result:Prolongedlungallograftsurvivalinadosedependentmanner.REFERENCES[1].NakashimaS,etal.AntiproliferativeeffectsofNKH477,aforskolinderivative,oncytokineprofileinratlungallografts.JHeartLungTransplant.2005Apr;24(4):462-9.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:40