Facinicline-hydrochloride-RG3487-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEFaciniclinehydrochlorideCat.No.:HY-108057ACASNo.:677305-02-1Synonyms:RG3487hydrochloride分?式:C??H??ClN?O分?量:306.79作?靶點:nAChR;5-HTReceptor作?通路:MembraneTransporter/IonChannel;NeuronalSignaling;GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(407.44mM;Needultrasonic)Methanol:25mg/mL(81.49mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.2596mL16.2978mL32.5956mL5mM0.6519mL3.2596mL6.5191mL10mM0.3260mL1.6298mL3.2596mL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備液，并請注意儲備液的保存?式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲備液可以根據(jù)儲存條件，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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥6.25mg/mL(20.37mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥6.25mg/mL(20.37mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥6.25mg/mL(20.37mM);ClearsolutionBIOLOGICALACTIVITY?物活性Faciniclinehydrochloride(RG3487hydrochloride)具有?服活性的煙堿α7receptor部分激動劑，對?nAChR的Ki值為6nM。Faciniclinehydrochloride(RG3487hydrochloride)可改嚙齒類動物的認(rèn)知和感覺運(yùn)動門控。Faciniclinehydrochloride(RG3487hydrochloride)對5-HT3受體(拮抗劑)的Ki值為1.2nM。IC50&Target5-HT3Receptorα71.2nM(Ki)6nM(Ki)體外研究Facinicline(RG3487)activateshumanα7nAChRswithanEC50of0.8μM(oocytes)and7.7μM(QM7cells)[1].Facinicline(RG3487)exhibitsantagonistpropertiesattheserotonin3receptor(IC502.8nM(oocytes),32.7nM(N1E-115cells))[1].體內(nèi)研究Facinicline(RG3487)improvesobjectrecognitionmemoryinratsafteracute[minimallyeffectivedose(MED)1.0mg/kgp.o.]orrepeated(10day)administrationatbrainandplasmaconcentrationsinthelow-nanomolarrange[1].RG3487(0.1–10mg/kgp.o.)selectivelyenhancesobjectrecognitionmemory[1].AnimalModel:MaleSprague-Dawleyrats[1].Dosage:0.1-10mg/kg(PharmacokineticAnalysis).Administration:Orally.Result:ThemeanCmaxwastypicallyobservedbetween0.5and4h.REFERENCES[1].TanyaLWallace,etal.RG3487,aNovelNicotinicα7ReceptorPartialAgonist,ImprovesCognitionandSensorimotorGatinginRodents.JPharmacolExpTher.2011Jan;336(1):242-53.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For