Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETRPM8antagonist2Cat.No.:HY-112430CASNo.:259674-19-6分?式:C??H??N?O?分?量:398.5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:160mg/mL(401.51mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.5094mL12.5471mL25.0941mL5mM0.5019mL2.5094mL5.0188mL10mM0.2509mL1.2547mL2.5094mL請(qǐng)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(qǐng)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(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)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(qǐng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.67mg/mL(6.70mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.67mg/mL(6.70mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.67mg/mL(6.70mM);ClearsolutionBIOLOGICALACTIVITY?物活性TRPM8antagonist2?種有效的，選擇性的TRPM8拮抗劑，IC50值為0.2nM，可?于研究神經(jīng)性疼痛綜合癥。IC50&TargetIC50:0.2nM(TRPM8)[1]體外研究TRPM8antagonist2(Compound14)isapotentandselectiveTRPM8antagonist,withanIC50of0.2nM,usedintheresearchofneuropathicpainsyndromes.TRPM8antagonist2potentlyinhibitsmenthol-inducedincreaseinintracellularCa2+levelsinCa2+fluorimetricassaysinHEK293cellsstablyexpressingtheratisoformofTRPM8channels(IC50,40nM)[1].體內(nèi)研究TRPM8antagonist2(1,10,and30mg/kg,s.c.)showsamarked,dose-dependentantinociceptiveactivity,andinhibitswet-dogshakes(WDS)-likecoldhypersensitivityinmiceby63%at30mg/kg.Inaddition,TRPM8antagonist2(0.1and1μg,s.c.)attenuatesOxaliplatin(OXP)-inducedcoldallodyniainmice[1].PROTOCOLAnimalMice[1]Administration[1]Icilin,aTRPM8agonist,isdissolvedin20%DMSOand1%Tween80indistilledwaterandinjectedintraperitoneally(i.p.)inavolumeof10mL/kg.Eachanimalisacclimatizedfor30minfortwoconsecutivedaysbeforeicilinadministration.TRPM8antagonist2(compound14)stockispreparedinDMSOanddilutedinsalineforinjections.Gabapentinisdissolvedinsalineandadministereds.c.atthedoseof25mg/kg60minpriortoicillininjection.Controlanimalsreceivethevehicleinjection[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].BertaminoA,etal.IdentificationofaPotentTryptophan-BasedTRPM8AntagonistWithinVivoAnalgesicActivity.JMedChem.2018Jul10.doi:10.1021/acs.jmedchem.8b00545.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical