MDR-652-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEMDR-652Cat.No.:HY-136363CASNo.:1933528-96-1分?式:C??H??ClFN?O?S分?量:447.95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:250mg/mL(558.10mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2324mL11.1620mL22.3239mL5mM0.4465mL2.2324mL4.4648mL10mM0.2232mL1.1162mL2.2324mL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，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。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，配制前請(qǐng)先配制澄的儲(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，體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥6.25mg/mL(13.95mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥6.25mg/mL(13.95mM);ClearsolutionBIOLOGICALACTIVITY1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE?物活性MDR-652?種?效的特異性瞬時(shí)受體電位?草酸亞型1(TRPV1)配體，具有激動(dòng)劑活性。對(duì)hTRPV1和rTRPV1的Ki分別為11.4和23.8nM。對(duì)hTRPV1和rTRPV1的EC50分別為5.05和93nM。具有局部鎮(zhèn)痛作?[1]。IC50&TargethTRPV1rTRPV1hTRPV1rTRPV111.4nM(Ki)23.8nM(Ki)5.05nM(EC50)93nM(EC50)體內(nèi)研究MDR-652(0.5and5mg/kg)displaysadose-dependentdecreaseofbodytemperature,supportingthatMDR-652displaysTRPV1agonismintheintactanimal[1].MDR-652(5-10mg/kg;i.p.ands.c.)blockstheneuropathicpaincompletely,indicating100%maximumpossibleeffect(MPE)[1].MDR-652hasapromisingtopicalpharmacokineticprofile[1].MDR-652hasnosignificanttoxicity.Inasingle-dosetoxicitystudy,theLD50ofMDR-652ishigherthan200and2000mg/kgini.p.andp.o.administration,respectively[1].AnimalModel:ICRmouse[1]Dosage:0.5and5mg/kgAdministration:Administeredintraperitoneally;7hoursResult:Decreasedbodytemperatureinadose-dependentmanner.AnimalModel:Ratswithspinalnerveligation(SNL)model[1]Dosage:1,2,5,and10mg/kgAdministration:Administeredintraperitoneallyandsubcutaneously;24hoursResult:Thei.p.administrationexhibitedanexcellentanddosedependentanalgesicprofilewithanED50of0.5-2mg/kg.Thesubcutaneousinjection(sc)alsodisplayedanexcellentanalgesicoutcomewithmaximumeffectat30minafteradministration.REFERENCES[1].JihyaeAnn,etal.DiscoveryofNonpungentTransientReceptorPotentialVanilloid1(TRPV1)AgonistasStrongTopicalAnalgesic.JMedChem.2020Jan9;63(1):418-424.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical/r/