Syk-Inhibitor-II-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemESykInhibitorIICat.No.:HY-112390ACASNo.:726695-51-8分⼦式:C₁₄H₁₅F₃N₆O分⼦量:340.3作⽤靶点:Syk;5-HTReceptor作⽤通路:ProteinTyrosineKinase/RTK;GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:5mg/mL(14.69mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.9386mL14.6929mL29.3858mL5mM0.5877mL2.9386mL5.8772mL10mM0.2939mL1.4693mL2.9386mL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，并请注意储备液的保存⽅式和期限。BIOLOGICALACTIVITY⽣物活性SykInhibitorII⼀种有效的，⾼选择性和ATP竞争性Syk抑制剂，IC50为41nM。SykInhibitorII抑制RBL细胞释放5-HT，IC50为460nM。SykInhibitorII对其他激酶的作⽤较⼩，并具有抗过敏作⽤。IC50&TargetserotoninSykPKCεPKCβ2460nM(IC50)41nM(IC50)5.1μM(IC50)11μM(IC50)ZAP-70BtkItk1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE11.2μM(IC50)15.5μM(IC50)22.6μM(IC50)体外研究SykInhibitorII(compound9a)showslesspotentagainstPKCε,PKCβ2,ZAP-70,Btk,andItkwithIC50valuesof5.1µM,11µM,11.2µM,15.5µM,and22.6µM,respectively[1].体内研究SykInhibitorII(Compound9a;10-100mg/kg)issubcutaneouslyadministeredtomice30minbeforeantigenchallenge.SykInhibitorIIinhibitstheanaphylaxisreactiondose-dependentlywithanID50valueof13.2mg/kg[1].REFERENCES[1].HiroyukiHisamichi,etal.SyntheticstudiesonnovelSykinhibitors.Part1:Synthesisandstructure-activityrelationshipsofpyrimidine-5-carboxamidederivatives.BioorgMedChem.2005Aug15;13(16):4936-51.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-