iGOT1-01-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEiGOT1-01Cat.No.:HY-124825CASNo.:882256-55-5分?式:C??H??N?O分?量:320.39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:100mg/mL(312.12mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.1212mL15.6060mL31.2120mL5mM0.6242mL3.1212mL6.2424mL10mM0.3121mL1.5606mL3.1212mL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(7.80mM);Clearsolution1/2MasterofBioactiveMolecules—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(7.80mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.80mM);ClearsolutionBIOLOGICALACTIVITY?物活性iGOT1-01有效的天冬氨酸轉(zhuǎn)氨酶1(?氨酸草酰?酸轉(zhuǎn)氨酶1；GOT1)抑制劑，在MDH偶聯(lián)GOT1酶法測(cè)定中IC50為85μM，在GOT1/GLOX/HRP測(cè)定中IC50為11.3μM。iGOT1-01具有抗癌活性。IC50&TargetIC50:85μM(MDHcoupledGOT1enzymaticassay)and11.3μM(GOT1/GLOX/HRPassay)[1]體外研究iGOT1-01hasanIC50of84.6μMintheGOT1/MDH1assay.NoinhibitoryactivityisobservedforiGOT1-01againstMDH1aloneat100μM[2].iGOT1-01(3.125-200μM;for3h)revealslittletonotoxicityusingtworeadoutsofcellviabilityinPaTu8902pancreaticandDLD1coloncancercells[2].體內(nèi)研究iGOT1-01(compound1a;20mg/kg;oral)hasreasonablebioavailabilityandexposureproperties(t1/2=0.7hours,Cmax=4133ng/mL,AUC(0-24hours)=11734hour?ng/mL)[1].AnimalModel:FemaleCD1micewith9weeksold[1]Dosage:20mg/kg(PharmacokineticAnalysis)Administration:OralResult:Hasreasonablebioavailabilityandexposureproperties(t1/2=0.7hours,Cmax=4133ng/mL,AUC(0-24hours)=11734hour?ng/mL).REFERENCES[1].JustinAnglin,etal.Discoveryandoptimizationofaspartateaminotransferase1inhibitorstotargetredoxbalanceinpancreaticductaladenocarcinoma.BioorgMedChemLett.2018Sep1;28(16):2675-2678.[2].MelissaCHolt,etal.BiochemicalCharacterizationandStructure-BasedMutationalAnalysisProvideInsightintotheBindingandMechanismofActionofNovelAspartateAminotransferaseInhibitors.Biochemistry.2018Nov27;57(47):6604-6614.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications