Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEFK614Cat.No.:HY-101292CASNo.:193012-35-0分?式:C??H??Cl?N?O?S分?量:468.4作?靶點(diǎn):PPAR作?通路:CellCycle/DNADamage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(213.49mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1349mL10.6746mL21.3493mL5mM0.4270mL2.1349mL4.2699mL10mM0.2135mL1.0675mL2.1349mL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；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)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(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%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.34mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性FK614?種?服活性?噻唑烷?酮(TZD)型選擇性PPARγ調(diào)節(jié)劑(SPPARM)。FK614?種PPARγ激動(dòng)劑，顯?出強(qiáng)?的抗糖尿病活性。FK614在脂細(xì)胞分化的各個(gè)階段對(duì)PPARγ的激活有不同的響。FK614可?于研究??糖、??油三酯?癥、糖耐量異常和2型糖尿病。IC50&TargetPPAR-γ體外研究FK614(0.1~10000nM;24hours;CV-1cells)activatesPPARγ-dependenttranscriptioninaconcentration-dependentmanner.FK614(0~0.1μM;5days;3T3-L1adipocytes)makestriglyceridecontentincreasedinaconcentration-dependentmanner.FK614hasdifferenteffectsontheactivationofPPARγateachstageofadipocytedifferentiation[1].FK614isaninsulinsensitizerpotentiallyfortreatmentofpostherpeticneuralgia.FK614isanon-TZDinsulinsensitizer[2].體內(nèi)研究FK614(0.32~3.2mg/kg;p.o.;14days)dose-dependentlyreducesplasmaglucoselevel[3].FK614(0.1~10mg/kg;p.o.;14days)improvestheimpairedglucosetolerance[3].AnimalModel:db/dbMiceDosage:0.1~10mg/kgAdministration:P.o.Result:Improvedtheimpairedglucosetolerance.AnimalModel:db/dbMiceDosage:0.32~3.2mg/kgAdministration:P.o.Result:Dose-dependentlyreducedplasmaglucoselevel.REFERENCES[1].FujimuraT,etal.Aselectiveperoxisomeproliferator-activatedreceptorgammamodulatorwithdistinctfatcellregulationproperties.JPharmacolExpTher.2006;318(2):863-871.[2].FujimuraT,etal.FK614,anovelperoxisomeproliferator-activatedreceptorgammamodulator,inducesdifferentialtransactivationthroughauniqueligand-specificinteractionwithtranscriptionalcoactivators.JPharmacolSci.2005;99(4):342-352.[3].MinouraH,etal.AmelioratingeffectofFK614,anovelnonthiazolidinedioneperoxisomeproliferator-activatedreceptorgammaagonist,oninsulinresistanceinZuckerfattyrat.EurJPharmacol.2005;519(1-2):182-190.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalappl