TDI-10229-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETDI-10229Cat.No.:HY-132298分⼦式:C₁₆H₁₆ClN₅分⼦量:313.78作⽤靶点:AdenylateCyclase作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(398.37mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1869mL15.9347mL31.8695mL5mM0.6374mL3.1869mL6.3739mL10mM0.3187mL1.5935mL3.1869mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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(6.63mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.63mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性TDI-10229⼀种⼝服有效的可溶性腺苷酸环化酶(sAC,ADCY10)抑制剂(IC50值为195nM)。TDI-10229在⽣化和细胞分析中都显⽰出对sAC的纳尔级抑制，并表现出⾜以保证其⽤作体内⼯具化合物的⼩⿏药代动⼒学特性[1][2]。IC50&TargetIC50:195nM(sAC)[2].体外研究TDI-10229exhibitsgoodpermeabilitywithanIC50of92nMforhuman4-4cells[2].体内研究TDI-10229(5mg/kg;p.o.)treatmentshowstheCmax,AUCandMRTwere15.5μM,94μgh/mLand3.95hours,respectively.AnimalModel:Mouse[2]Dosage:20mg/kgAdministration:P.o.(PharmacokineticAnalysis)Result:TheCmax,AUCandMRTwere15.5μM,94μgh/mLand3.95hours,respectively.REFERENCES[1].BalbachM,etal.Solubleadenylylcyclaseinhibitionpreventshumanspermfunctionsessentialforfertilization[publishedonlineaheadofprint,2021Aug31].MolHumReprod.2021;gaab054.[2].FushimiM,etal.DiscoveryofTDI-10229:APotentandOrallyBioavailableInhibitorofSolubleAdenylylCyclase(sAC,ADCY10).ACSMedChemLett.2021;12(8):1283-1287.Published2021Jul14.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: