TM-N1324-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETM-N1324Cat.No.:HY-108699CASNo.:1144477-35-9分?式:C??H??ClFN?O分?量:397.79作?靶點(diǎn):GHSR作?通路:GPCR/GProtein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:12.22mg/mL(30.72mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.5139mL12.5694mL25.1389mL5mM0.5028mL2.5139mL5.0278mL10mM0.2514mL1.2569mL2.5139mL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:1.22mg/mL(3.07mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—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:≥1.22mg/mL(3.07mM);ClearsolutionBIOLOGICALACTIVITY?物活性TM-N1324G蛋?偶聯(lián)受體39(GPR39)的激動(dòng)劑，在Zn2+存在的情況下，對(duì)?和?GPR39的EC50值分別為9nM和5nM，在Zn2+不存在的情況下，對(duì)?和?GPR39的EC50值分別為280nM和180nM。IC50&TargetEC50:280nM(humanGPR39withoutZn2+),9nM(humanGPR39withZn2+),180nM(murineGPR39withoutZn2+),5nM(murineGPR39withZn2+)[1]體外研究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