Samelisant-SUVN-G3031-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESamelisantCat.No.:HY-120124CASNo.:1394808-20-8Synonyms:SUVN-G3031分?式:C??H??Cl?N?O?分?量:446.41作?靶點(diǎn):HistamineReceptor作?通路:GPCR/GProtein;Immunology/Inflammation;NeuronalSignaling儲存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:62.5mg/mL(140.01mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2401mL11.2005mL22.4009mL5mM0.4480mL2.2401mL4.4802mL10mM0.2240mL1.1200mL2.2401mL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；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(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?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.66mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.66mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.66mM);ClearsolutionBIOLOGICALACTIVITY?物活性Samelisant(SUVN-G3031)?種?服有效的，可通過?腦屏障的選擇性組胺H3受體(H3R)反向激動(dòng)劑。Samelisant對?類(hH3R;Ki=8.7nM)和??(rH3R;Ki=9.8nM)H3R具有相似的結(jié)合親和?，表明沒有種間差異。Samelisant可?于研究睡眠相關(guān)疾病[1]。體外研究SamelisantdisplaysinverseagonistactivityanditexhibitsveryhighselectivitytowardsH3R.ThepEC50valueofhistamine(8.5)forhumanH3receptorincreasesto8.2,7.3and6.2aftertreatmentwith1,10and100nMofSamelisant,respectively.ThepEC50valueofhistamine(8.2)forratH3receptorincreasesto7.9,7.4and6.4aftertreatmentwith1,10and100nmol/LofSamelisant,respectively[1].SamelisantbindstotheorthostericsiteinareversiblemannerwithKbvaluesof1.3nMand1.1nMdeducedfrompA2valueforhumanandratH3R,respectively[1].Samelisantalsomodulatesdopamineandnorepinephrinelevelsinthecerebralcortexwhileithasnoeffectsondopaminelevelsinthestriatumornucleusaccumbens[1].體內(nèi)研究TreatmentwithSamelisant(10and30mg/kg,p.o.)producesasignificantincreaseinwakefulnesswithaconcomitantdecreaseinnon-rapideyemovementsleep(NREM)sleepinorexinknockoutmicesubjectedtosleepelectroencephalography(EEG)[1].Samelisantalsoproducesasignificantdecreaseindirectrapideyemovement(REM)sleeponset(DREM)episodes,demonstratingitsanticataplecticeffectsinananimalmodelrelevanttonarcolepsy[1].Samelisanttreatmentinmiceproducesadose-dependentincreaseintele-methylhistaminelevelsindicatingtheactivationofhistaminergicneurotransmission[1].AnimalModel:MaleWistarratsormaleC57BL6Jmice[1]Dosage:1,3,10,and30mg/kgAdministration:OraladministrationResult:Producedadose-dependentincreaseint-MHlevelsinthefrontalcortex,hypothalamusandcerebrospinalfluid(CSF)ofmaleWistarrats.Producedasignificantincreaseint-MHlevelsofthefrontalcortex,striatumandhypothalamusinmice.REFERENCES[1].RamakrishnaNirogi,etal.Samelisant(SUVN-G3031),apotent,selectiveandorallyactivehistamineH3receptorinverseagonistforthepotentialtreatmentofnarcolepsy:pharmacologicalandneurochemicalcharacterisation.Psychopharmacology(Berl).20212/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnot