BAY-36-7620-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEBAY36-7620Cat.No.:HY-107513CASNo.:232605-26-4分子式:C??H??O?分子量:278.35作用靶點(diǎn):mGluR作用通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性BAY36-7620是有效的，非競(jìng)爭(zhēng)性的并且有反向激動(dòng)劑活性的mGlu1Receptor的拮抗劑(IC50為0.16μM)。BAY36-7620通過(guò)抑制mGlu1受體來(lái)抑制腫瘤生長(zhǎng)并延長(zhǎng)腫瘤小鼠壽命。BAY36-7620抑制A549腫瘤中的AKT磷酸化。BAY36-7620對(duì)急性硬膜下血腫大鼠模型具有神經(jīng)保護(hù)作用。BAY36-7620可用于非小細(xì)胞肺癌和乳腺癌研究[1][2][3][4]。IC50&TargetmGluR1mGluR1amGluR2mGluR50.16μM(IC50)0.38μM(IC50)0.14μM(IC50)0.24μM(IC50)體外研究BAY36-7620(0.1-10μM)completelyinhibitsmGlu1receptors10μMinHEK293Cells[1].BAY36-7620(10-25μM,4days)reducescellproliferationandinhibitstumor-relatedproteinexpressioninA549cells[2].BAY36-7620(72h)inhibitsMCF-7,T-47D,BT-474,MDA-MB-231,Hs578TandBT-549cellgrowthandproliferationwithIC50sof27.7,37.1,20.8,41.0,21.0and15.7μM,respectively[3].BAY36-7620(25-50μM,24-72h)causesDNAdamageandinducesmodestG2/MarrestinT-47D,BT-474,MDA-MB-231,andBT-549celllines[3].WesternBlotAnalysis[2]CellLine:A549celllineConcentration:10,25μMIncubationTime:Overnight1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEResult:EnhancedtheexpressionofcleavedPARPandreducedbcl-2proteinexpression.ReducedtheexpressionofHIF-1αproteinandHIFactivity.ReducedthesecretionofVEGFandIL-8intosupernatants.CellProliferationAssay[3]CellLine:TMCF-7,T-47D,BT-474,MDA-MB-231,Hs578TandBT-549celllineConcentration:50μMIncubationTime:72hResult:Decreasedthepercentageofproliferatingcellsinallbreastcancercellline.體內(nèi)研究BAY36-7620(5-10mg/kgfori.p;oncedailyfor24days)inhibitstumorgrowthandprolongsthesurvivalofLungtumorsmicemodel[2].BAY36-7620(0.01-0.03mg/kgfori.v.;4h)hasneuroprotectiveeffectinacutesubduralhematomaratmodel[4].AnimalModel:Lungtumorsmicemodel[2]Dosage:5,10mg/kgAdministration:Intraperitonealinjection(i.p.);Oncedailyfor24daysResult:Suppressedtumorgrowthinathymicmicewithlungtumors.Prolongedthesurvivalofinoculatedmicewhencomparedtocontrolgroup.DecreasedthelevelofAKTphosphorylationinA549tumors.AnimalModel:Subduralhematomaratmodel[4]Dosage:0-3mg/kgAdministration:Intravenousinjection(i.v.);4hResult:Hadneuroprotectiveeffectwiththeefficacyof40–50%at0.01and0.03mg/kg.REFERENCESCarrollFY,etal.BAY36-7620:apotentnon-competitivemGlu1receptorantagonistwithinverseagonistactivity.MolPharmacol.2001May;59(5):965-73.XiaH,etal.Inhibitionofmetabotropicglutamatereceptor1suppressestumorgrowthandangiogenesisinexperimentalnon-smallcelllungcancer.EurJPharmacol.2016Jul15;783:103-11.DolfiSC,etal.Riluzoleexertsdistinctantitumoreffectsfromametabotropicglutamatereceptor1-specificinhibitoronbreastcancercells.Oncotarget.2017Jul4;8(27):44639-44653.2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEDeVryJ,etal.NeuroprotectiveandbehavioraleffectsoftheselectivemetabotropicglutamatemGlu(1)receptorantagonistBAY36-7620.EurJPharmacol.2001Oct5;428(2):203-14.McePdfHeightCaution:Producthasnotbeenfully