TM-N1324-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETM-N1324Cat.No.:HY-108699CASNo.:1144477-35-9分⼦式:C₁₈H₁₃ClFN₇O分⼦量:397.79作⽤靶点:GHSR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:12.22mg/mL(30.72mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5139mL12.5694mL25.1389mL5mM0.5028mL2.5139mL5.0278mL10mM0.2514mL1.2569mL2.5139mL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:1.22mg/mL(3.07mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1.22mg/mL(3.07mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性TM-N1324G蛋⽩偶联受体39(GPR39)的激动剂，在Zn2+存在的情况下，对⼈和⿏GPR39的EC50值分别为9nM和5nM，在Zn2+不存在的情况下，对⼈和⿏GPR39的EC50值分别为280nM和180nM。IC50&TargetEC50:280nM(humanGPR39withoutZn2+),9nM(humanGPR39withZn2+),180nM(murineGPR39withoutZn2+),5nM(murineGPR39withZn2+)[1]体外研究TM-N1324activateshumanGPR39withhighefficacyandpotenciesof280nMand9nMintheabsenceandpresenceofZn2+,respectively.TM-N1324hassimilarpotenciesonmurineGPR39,180nMand5nM.TM-N1324isalsofoundtohavepromisinginvitroADMEproperties.TM-N1324hasreasonablygoodaqueoussolubility(65μMatpH7.0).MeasurementsofsomatostatinconfirmsthattheGPR39agonistTM-N1324increasessomatostatinreleaseby53%[1].PROTOCOLCellAssayCaco-2cellsareusedasaninvitromodelofthehumanintestinalepitheliumandpermitassessmentoftheintestinalpermeabilityofTM-N1324.TM-N1324isaddedtoeithertheapicalorbasolateralsideofaconfluentmonolayerofCaco-2cellsandpermeabilityismeasuredbymonitoringtheappearanceoftheTM-N1324ontheoppositesideofthemembraneusingLC-MS/MS.TM-N1324(3µM)isincubatedwithpooledlivermicrosomesandincubatedat5timepointsoverthecourseofa45minexperimentfinallyTM-N1324isanalyzedbyLC-MS/MS.Theintrinsicclearance(CLint)andt1/2valuesforTM-N1324inhumanandmousemicrosomesarereported[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].FrimurerTM,etal.Model-BasedDiscoveryofSyntheticAgonistsfortheZn2+-SensingG-Protein-CoupledReceptor39(GPR39)RevealsNovelBiologicalFunctions.JMedChem.2017Feb9;60(3):886-898.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical