Linopirdine-DuP-996-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemELinopirdineCat.No.:HY-W020468CASNo.:105431-72-9Synonyms:DuP996分?式:C??H??N?O分?量:391.46作?靶點(diǎn):PotassiumChannel;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(319.32mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.5545mL12.7727mL25.5454mL5mM0.5109mL2.5545mL5.1091mL10mM0.2555mL1.2773mL2.5545mL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:≥2.08mg/mL(5.31mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.31mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoil1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(5.31mM);ClearsolutionBIOLOGICALACTIVITY?物活性Linopirdine(DuP996)?種具有?服活性的，選擇性M型K+電流(IM；Kv7；KCNQChannels)抑制劑，IC50為2.4μM。LinopirdineTRPV1激活劑。Linopirdine?種公認(rèn)的認(rèn)知增強(qiáng)藥物，可增加??腦組織中?酰膽堿的釋放。IC50&TargetIC50:2.4μM(M-typeK+current)[1]體外研究Linopirdine(DuP996)inhibitsIC(measuredasamediumafterhyperpolarizationtailcurrent,ImAHP)withanIC50of16.3μM.Linopirdine(100μM)weaklyinhibitstheK+leakcurrent,IL,thetransientoutwardcurrent,IA,thedelayedrectifier,IK,andtheslowcomponentofIAHP,by28,37,36and52percent,respectively.ThemixedNa+/K+inwardrectifyingcurrent,IQ,isessentiallyunaffectedbyLinopirdine(IC50>300μM)[1].LinopirdineactsasanagonistofTRPV1(transientreceptorpotentialvanilloidtype1)[3].體內(nèi)研究Linopirdine(DuP996;i.v.;0.1-6mg/kg;increasingdoses)transiently(10-15min)anddose-dependentlyincreasesMAPbyupto15%[2].AnimalModel:MaleSprague-Dawleyrats(300-350g)[2]Dosage:0.1,0.5,1,3,6mg/kgAdministration:5intravenousbolusinjectionsofincreasingdosesResult:Transientlyanddose-dependentlyincreasesMAPbyupto15%.REFERENCES[1].SchneeME,etal.Selectivityoflinopirdine(DuP996),aneurotransmitterreleaseenhancer,inblockingvoltage-dependentandcalcium-activatedpotassiumcurrentsinhippocampalneurons.JPharmacolExpTher.1998Aug;286(2):709-17.[2].NassoiySP,etal.Kv7voltage-activatedpotassiumchannelinhibitorsreducefluidresuscitationrequirementsafterhemorrhagicshockinrats.JBiomedSci.2017Jan17;24(1):8.[3].NeacsuC,etal.TheM-channelblockerlino