JNJ-54175446-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEJNJ-54175446Cat.No.:HY-117508CASNo.:1627902-21-9分⼦式:C₁₈H₁₃ClF₄N₆O分⼦量:440.78作⽤靶点:P2XReceptor作⽤通路:MembraneTransporter/IonChannel储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:62.5mg/mL(141.79mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2687mL11.3435mL22.6871mL5mM0.4537mL2.2687mL4.5374mL10mM0.2269mL1.1344mL2.2687mL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。-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。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.72mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.72mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.72mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性JNJ-54175446⼀种有效、选择性、可透过⾎脑屏障的P2X7受体拮抗剂，对⼈和⼤⿏的P2X7受体的pIC50值分别为8.46和8.81。IC50&TargetpIC50:8.46(hP2X7receptor),8.81(rP2X7receptor)[1]体外研究JNJ-54175446(Compound14)isapotentandselectivebrainpenetrantP2X7antagonist,withpIC50sof8.46and8.81forhP2X7andrP2X7,respectively.JNJ-54175446showslesspotentactivityagainstmouse,dogandMacaqueP2X7(pIC50,7.8,7.9and8.1,respectively)[1].体内研究JNJ-54175446showsdose-dependentoccupancywiththeED50of0.46mg/kg,correspondingtoplasmaEC50of105ng/mL[1].REFERENCES[1].LetavicMA,etal.4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-BasedP2X7ReceptorAntagonists:OptimizationofPharmacokineticPropertiesLeadingtotheIdentificationofaClinicalCandidate.SendtoMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:40