GW788388-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGW788388Cat.No.:HY-10326CASNo.:452342-67-5分?式:C??H??N?O?分?量:425.48作?靶點(diǎn):TGF-βReceptor作?通路:TGF-beta/Smad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:25mg/mL(58.76mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.3503mL11.7514mL23.5029mL5mM0.4701mL2.3503mL4.7006mL10mM0.2350mL1.1751mL2.3503mL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:≥2.5mg/mL(5.88mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.88mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.88mM);ClearsolutionBIOLOGICALACTIVITY?物活性GW788388?種有效的ALK5抑制劑，IC50值18nM；同時(shí)抑制TGF-βII型受體和激活素II型受體的活性，但對(duì)BMPII型受體?作?。IC50&TargetIC50:18nM(ALK5)體內(nèi)研究GW788388givenorallyfor5weekssignificantlyreducesrenalfibrosisanddecreasedthemRNAlevelsofkeymediatorsofextracellularmatrixdepositioninkidneysindb/dbmice[1].GW788388(50mg/kg/day,p.o.)significantlyattenuatessystolicdysfunctionintheMIanimals,togetherwiththeattenuationoftheactivated(phosphorylated)Smad2(P<0.01),α-smoothmuscleactin(P<0.001),andcollagenI(P<0.05)inthenoninfarctzoneofMIrats[2].GW788388reducestheexpressionofcollagenIA1by80%atadoseof1mg/kgtwiceaday(b.i.d.).GW788388significantlyreducestheexpressionofcollagenIA1mRNAwhenadministeredorallyat10mg/kgonceaday(u.i.d.)inamodelofpuromycinaminonucleoside-inducedrenalfibrosis[3].PROTOCOLAnimalOneweekpostsurgery,sham-operated(N=6)andinfarctedanimals(N=10)arerandomizedtotreatmentwithAdministration[2]theALK5inhibitorGW788388(GSK)atadosageof50mg/kg/daybygavage,whichhasbeenshowntosignificantlyattenuatecollagenoverexpressioninarodentmodelofdimethylnitrosamine-inducedliverdisease.Untreatedrats,thatis,sham-operated(N=9)andMIanimals(N=15),aregavagedwithvehicle(1%carboxymethylcellulosesolution).Fouranimalswith<25%infarctsizeasdeterminedpostmortembyhistologyareexcludedfromfurtheranalyses.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CellProlif.2021Jan;54(1):e12933.?IntJMolSci.2022,23(20),12219.?OrgLett.2020Aug7;22(15):5726-5730.?OrgLett.2017Jan6;19(1):286-289.?LabInvest.2019Jul;99(8):1173-1192.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].PetersenM,etal.OraladministrationofGW788388,aninhibitorofTGF-betatypeIandIIreceptorkinases,decreasesrenalfibrosis.KidneyInt,2008,73(6),705-715.[2].TanSM,etal.Targetedinhibitionofactivinreceptor-likekinase5signalingattenuatescardiacdysfunctionfollowingmyocardialinfarction.AmJPhysiolHeartCircPhysiol,2010,298(5),H1415-1425.[3].GellibertF,etal.Discoveryof4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H-pyran-4-yl)benzamide(GW788388):apotent,selective,andorallyactivetransforminggrowthfactor-betatypeIreceptorinhibitor.JMedChem.2006,49McePdfHeightCaution:Produ