Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPF-05105679Cat.No.:HY-115506CASNo.:1398583-31-7分?式:C??H??FN?O?分?量:428.45作?靶點(diǎn):TRPChannel作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(291.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.3340mL11.6700mL23.3399mL5mM0.4668mL2.3340mL4.6680mL10mM0.2334mL1.1670mL2.3340mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.85mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.85mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.85mM);ClearsolutionBIOLOGICALACTIVITY?物活性PF-05105679?種具有?服活性的，選擇性TRPM8拮抗劑，IC50為103nM。PF-05105679有?于感冒相關(guān)疼痛的潛?。IC50&TargetTRPM8103nM(IC50)體外研究PF-05105679demonstrates>100-foldselectivityacrossarangeofdifferentreceptors,ionchannels,andenzymesincludingthecloselyrelatedTRPV1andTRPA1channels[1].TRPM8,alsoknownasthecoldandmentholreceptor1(CMR1),isamemberofthemelastatinsubfamily[1].體內(nèi)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