PF-05105679-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPF-05105679Cat.No.:HY-115506CASNo.:1398583-31-7分⼦式:C₂₆H₂₁FN₂O₃分⼦量:428.45作⽤靶点:TRPChannel作⽤通路:MembraneTransporter/IonChannel;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(291.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3340mL11.6700mL23.3399mL5mM0.4668mL2.3340mL4.6680mL10mM0.2334mL1.1670mL2.3340mL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(4.85mM);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(4.85mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.85mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PF-05105679⼀种具有⼝服活性的，选择性TRPM8拮抗剂，IC50为103nM。PF-05105679有⽤于感冒相关疼痛的潜⼒。IC50&TargetTRPM8103nM(IC50)体外研究PF-05105679demonstrates>100-foldselectivityacrossarangeofdifferentreceptors,ionchannels,andenzymesincludingthecloselyrelatedTRPV1andTRPA1channels[1].TRPM8,alsoknownasthecoldandmentholreceptor1(CMR1),isamemberofthemelastatinsubfamily[1].体内研究PF-05105679(0.2mg/kgforivand20mg/kgfororalgavage)hasaT1/2of3.9hours,aCLof31mL/min/kg,andaVssof7.4L/kgfordogs[1].PF-05105679(2,20mg/kg)hasaT1/2of3.6hours,aCLof19.8mL/min/kg,andaVssof6.2L/kgforrats[1].AnimalModel:Malebeagledogs(weight10to15kg)[1]Dosage:0.2mg/kg(iv)or20mg/kg(oralgavage)(PharmacokineticAnalysis)Administration:IvororalgavageResult:HadaT1/2of3.9hours,aCLof31mL/min/kg,andaVssof7.4L/kgfordogs.REFERENCES[1].AndrewsMD,etal.DiscoveryofaSelectiveTRPM8AntagonistwithClinicalEfficacyinCold-RelatedPain.ACSMedChemLett.2015Jan30;6(4):419-24.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu