Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEXPC-6444Cat.No.:HY-128772CASNo.:2230144-21-3分?式:C??H??F?N?O?S?分?量:498.58作?靶點(diǎn):SodiumChannel作?通路:MembraneTransporter/IonChannel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(250.71mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0057mL10.0285mL20.0570mL5mM0.4011mL2.0057mL4.0114mL10mM0.2006mL1.0028mL2.0057mL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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.17mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.17mM);ClearsolutionBIOLOGICALACTIVITY?物活性XPC-6444?種?效的，亞型選擇性的，CNS-滲透性的NaV1.6抑制劑(對(duì)hNaV1.6的IC50=41nM)。XPC-6444也有效阻斷了NaV1.2(IC50=125nM)。XPC-6444具有抗驚厥活性。IC50&TargetIC50:41nM(hNaV1.6),125nM(hNaV1.2)[1]體外研究XPC-6444showshighselectivityoverNaV1.1andNaV1.5[1].體內(nèi)研究XPC-6444exhibitsgoodmetabolicstabilityinhumanlivermicrosomesandhepatocytes,andlowpotentialforMDR1mediatedefflux[1].REFERENCES[1].FockenT,etal.IdentificationofCNS-PenetrantArylSulfonamidesasIsoform-SelectiveNaV1.6InhibitorswithEfficacyinMouseModelsofEpilepsy.JMedChem.2019Oct3.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021