AZD6538-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAZD6538Cat.No.:HY-119282CASNo.:453566-30-8分⼦式:C₁₅H₆FN₅O分⼦量:291.24作⽤靶点:mGluR作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:4mg/mL(13.73mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.4336mL17.1680mL34.3359mL5mM0.6867mL3.4336mL6.8672mL10mM0.3434mL1.7168mL3.4336mL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(protectfromlight)。-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。BIOLOGICALACTIVITY⽣物活性AZD6538⼀种有效、选择性和脑渗透性的mGluR5负变构调节剂。AZD6538抑制DHPG(HY-12598A)刺激的表达⼤⿏或⼈类mGluR5的HEK细胞内Ca2+释放，对⼤⿏mGluR5和⼈类mGluR5的IC50值分别为3.2和13.4nM。AZD6538可⽤于神经性疼痛的研究[1]。IC50&TargetratmGluR5humanmGluR53.2±0.1nM(IC50)13.4±1.3nM(IC50)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体外研究AZD6538completelyreversestheglutamate-stimulated(EC80,80μM)phosphatidylinositolhydrolysisinhumanmGluR5-GHEKcellsinaconcentration-dependentmanner,withanIC50of51±3nM[1].REFERENCES[1].RaboissonP,etal.DiscoveryandcharacterizationofAZD9272andAZD6538-TwonovelmGluR5negativeallostericmodulatorsselectedforclinicaldevelopment.BioorgMedChemLett.2012Nov15;22(22):6974-9.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792a