A3334-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEA3334Cat.No.:HY-131448CASNo.:854171-31-6分?式:C??H??N?O?分?量:307.3作?靶點(diǎn):Others作?通路:Others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:250mg/mL(813.54mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.2541mL16.2707mL32.5415mL5mM0.6508mL3.2541mL6.5083mL10mM0.3254mL1.6271mL3.2541mL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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(6.77mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性A3051?種有效的和具有?服活性的CXXC5-DVL的抑制劑，IC50值為63.06nM。A3334可?于研究?脂飲?(HFD)和蛋氨酸-膽堿缺乏飲?(MCD)誘導(dǎo)的疾病，例如肥胖，糖尿病和NASH。詳細(xì)信息請(qǐng)參考專利?獻(xiàn)WO2020079569。IC50&TargetIC50:63.06nM(CXXC5-DVL)[1]體外研究A3334(1-10μM)efficientlyinhibitstheadipogenicdifferentiationof3T3-L1preadipocytesviatheWnt/β-eateninsignalingpathway[1].A3334(1-10μM;24h)enhancestheTOPFlashreporteractivityinHEK293-TOPcells[1].體內(nèi)研究A3334(25mg/kg;p.o.oncedailyfor16weeks)hasanti-obesityeffectsintheHFDmice,andhasnoeffectonmicefedwithnormaldiet[1].A3334(25mg/kg;p.o.oncedailyfor5days)significantlyreducesfastingglucoseandthelevelsofglucosetolerance(GTT)andinsulintolerance(ITT)inseruminmice[1].A3334(25mg/kg;p.o.oncedailyfor3weeks)significantlyabolisheshepatosteatosisandtheincreasedlevelsofalaninetransaminase(ALT)andaspartatetransaminase(AST)inmice[1].AnimalModel:MaleC57BL/6Nmice(6-week-old)arefedonthehighfatdie(HFD)for16weeks[1]Dosage:25mg/kgAdministration:P.o.dailyfor16weeksResult:NotobservedtheHFD-inducedbodyweightgainandabdominalobesity.ReducedtheleveloftriglycerideandtotalcholesterolandincreasedthelevelofHDL-cholesterol.Suppressedtheincreaseinadipocytecellsizesandenhancementofinflammation.REFERENCES[1].ChoiKY,et,al.Compositionsandmethodsforsuppressingand/ortreatingmetabolicdiseasesand/oraclinicalconditionthereof.WO2020079569.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forr