Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENKH477Cat.No.:HY-103193CASNo.:138605-00-2Synonyms:Colforsindapropatehydrochloride分?式:C??H??ClNO?分?量:546.09作?靶點(diǎn):AdenylateCyclase作?通路:GPCR/GProtein儲(chǔ)存?式:-20°C,storedundernitrogen,awayfrommoisture*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?。溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(228.90mM;Needultrasonic)H2O:20mg/mL(36.62mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.8312mL9.1560mL18.3120mL5mM0.3662mL1.8312mL3.6624mL10mM0.1831mL0.9156mL1.8312mL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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?.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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.81mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(3.81mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.81mM);ClearsolutionBIOLOGICALACTIVITY?物活性NKH477(Colforsindapropatehydrochloride)直接激活腺苷酸環(huán)化酶(adenylatecyclase)的催化單元并增加細(xì)胞內(nèi)cAMP。NKH477?種?喉素衍?物，主通過對(duì)舒張性?臟功能的有益作?來改??衰竭。NKH477在體內(nèi)抗增殖作?，可以抑制??原位肺同種異體移植物的急性排斥。IC50&TargetAdenylateCyclase[1]體內(nèi)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