AF-353-Ro-4-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAF-353Cat.No.:HY-14483CASNo.:865305-30-2Synonyms:Ro-4分⼦式:C₁₄H₁₇IN₄O₂分⼦量:400.21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:100mg/mL(249.87mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4987mL12.4934mL24.9869mL5mM0.4997mL2.4987mL4.9974mL10mM0.2499mL1.2493mL2.4987mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(6.25mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.25mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.25mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性AF-353(Ro-4)⼀种有效选择性、⼝服可利⽤的P2X3/P2X2/3受体拮抗剂,抑制⼈和⼤⿏P2X3的pIC50值为8.0，抑制⼈P2X2/3的pIC50值为7.3[1][2]。IC50&TargetpIC50:8.0(humanP2X3),8.0(ratP2X3),7.3(humanP2X2/3)[1]体外研究AF-353(Ro-4)isahighlypotentinhibitorofα,β-meATP-evokedintracellularcalciumfluxincelllinesexpressingrecombinantratandhumanP2X3andhumanP2X2/3channels[1].AF-353(Ro-4)alsoblockshumanP2X2/3channelfunctionwithmarginallyreducedpotencywithap50of7.3[1].体内研究AF-353(Ro-4)doesnotcompromiseoxygenlevelsorcardiacfunction[2].AF-353(Ro-4)(10mg/kg,20mg/kg;i.v.;for4-6hours)inhibitsthepurinergicresponseinbothnormalandspinalcord-injured(SCI)rats[2].AF-353(Ro-4)(10mg/kg,20mg/kg;i.v.;for4-6hours)alsoreducestheinter-contractileintervalinnormalbutnotinSCIrats;however,thefrequencyofnon-voiding(NVC)inSCIratsissignificantlyreduced[2].AnimalModel:FemaleSprague-Dawleyrats(250–300g)bearingSCI[2]Dosage:10mg/kg,20mg/kgAdministration:Intravenousinjection;intervalof90minutes,for4hoursto6hoursResult:SignificantlyreducedpurinergicresponseinbothnormalandSCIrats.REFERENCES[1].GeverJR,etal.AF-353,anovel,potentandorallybioavailableP2X3/P2X2/3receptorantagonist.BrJPharmacol.2010Jul;160(6):1387-1398.[2].MunozA,etal.Modulationofbladderafferentsignalsinnormalandspinalcord-injuredratsbypurinergicP2X3andP2X2/3receptors.BJUInt.2012Oct;110(8PtB):E409-414.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappli