G-1-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEG-1Cat.No.:HY-107216CASNo.:881639-98-1分?式:C??H??BrNO?分?量:412.28作?靶點:EstrogenReceptor/ERR作?通路:Others儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(121.28mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4255mL12.1277mL24.2554mL5mM0.4851mL2.4255mL4.8511mL10mM0.2426mL1.2128mL2.4255mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.06mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(6.06mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.06mM);ClearsolutionBIOLOGICALACTIVITY?物活性G-1?個?甾體，?親和?且有選擇性的GPR30激動劑，其Ki值為11nM。IC50&TargetKi:11nM(GPR30)[1]體外研究G-1isanonsteroidal,high-affinityandselectiveagonistofGPR30withaKiof11nM[1].TreatmentwithG-1(10μMand100μM)for48and72hsignificantlydecreasescellproliferation(P50valueforG-1iscalculatedtobe20μM.TreatmentofA549cellswithG-1ataconcentrationof20μMrevealsasignificantincreaseinapoptosis,consistentwithitsantiproliferativeeffect(P[2].CellcycleanalysisofH295Rcellsafter24hofG-1treatmentdemonstratesacellcyclearrestintheG2phase.ThepresenceofG-1increasesBaxexpressionwhiledecreasesBcl-2[3].體內(nèi)研究Theresultsat14dayspost-injuryshowthattheBassomousescale(BMS)scoresaresignificantlyhigherintheG-1groupcomparedwiththeothergroups(P0.05)[1].G-1administrationproducesastatisticallysignificantdecreaseintumorvolumefromday14posttreatment.Graftedtumorsharvestedafterthree-weektreatmentwithG-1showasignificantdecreaseintumorweightcomparetovehicletreatedanimals[3].PROTOCOLCellAssay[2]A549humanlungcancercellsaretreatedwithvariousconcentrations(10nM,100nM,1μM,10μMand100μM)ofG-1in96-wellplatesandincubatedfor48or72h.Followingincubation,MTTsolutionisaddedtoeachwellataconcentrationof0.5mg/mL,andincubatedfor4hat37°C.Attheendofthisperiod,100μLDMSOsolventisaddedtoeachwell.Theabsorbancevalues[opticaldensity(OD)]at570nmofthesolutionineachwellarereadusingaspectrophotometer[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalFour-week-oldnu/nu-ForkheadboxN1nufemalemiceareusedinthisstudy.H295Rcells,6×106,Administration[3]suspendedin100μLPBS,arecombinedwith30μLofMatrigel(4mg/mL)andinjectedsubcutaneouslyintheshoulderofeachanimal.Micearetreated21daysaftercellinjection,whentumorshavereachedanaveragevolumeofabout200mm3.AnimalsarerandomlyassignedtobetreatedwithvehicleorG-1ataconcentrationof2mg/kg/daily.Drugtolerabilityisassessedintumor-bearingmiceintermsof:a)lethaltoxicity,i.e.anydeathintreatedmiceoccurringbeforeanydeathincontrolmice;b)bodyweightlosspercentage=100-[(bodyweightondayx/bodyweightonday1)×100],wherexrepresentsadayduringthetreatmentperiod.Animalsaresacrificedbycervicaldislocation42daysaftercellinjection[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE戶使?本產(chǎn)品發(fā)表的科研?獻?CellDeathDis.2022Apr19;13(4):372.?CellDeathDiscov.2022Jul16;8(1):323.?LifeSci.2022May28;120676.?Phytomedicine.2020Mar;68:153146.?JCellPhysiol.2021May;236(5):3780-3788.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ChengQ,etal.G-1exertsneuroprotectiveeffectsthroughGprotein-coupledestrogenreceptor1followingspinalcordinjuryinmice.BiosciRep.2016Aug31;36(4).pii:e00373.[2].KurtAH,etal.Oxidative/antioxidativeenzyme-mediatedantiproliferativeandproapoptoticeffectsoftheGPER1agonistG-1onlungcancercells.OncolLett.2015Nov;10(5):3177-3182.[3].ChimentoA,etal.GPERagonistG-1decreasesadrenocorticalcarcinoma(ACC)cellgrowthinvitroandinvivo.Oncotarget.2015