GNE0877-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGNE0877Cat.No.:HY-15796CASNo.:1374828-69-9分?式:C??H??F?N?分?量:339.32作?靶點(diǎn):LRRK2作?通路:Autophagy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(736.77mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.9471mL14.7354mL29.4707mL5mM0.5894mL2.9471mL5.8941mL10mM0.2947mL1.4735mL2.9471mL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>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.13mM);Clearsolution1/3MasterofBioactiveMolecules—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(6.13mM);ClearsolutionBIOLOGICALACTIVITY?物活性GNE0877?種?選擇性，具有?服活性以及腦滲透的LRRK2的抑制劑，其IC50值為3nM，Ki值為0.7nM。GNE0877可?于神經(jīng)科學(xué)的研究。IC50&TargetIC50:3nM(LRRK2)[1]體外研究GNE0877(1μM;10-30min)showsgoodcellularpotencyinhumanlivermicrosomesandhepatocytes[1].CellViabilityAssay[1]CellLine:HumanlivermicrosomesandhepatocytesConcentration:1μMIncubationTime:10,20and30minResult:Exibitedlowturnoverandgoodvitrostabilityinhumanlivermicrosomesandhepatocyteswithnoglucuronidation.體內(nèi)研究GNE0877(10and50mg/kg;i.p.once)inhibitsLRRK2Ser1292autophosphorylation[1].AnimalModel:BACtransgenicmiceexpressinghumanLRRK2proteinwiththeG2019SParkinson’sdiseasemutation[1]Dosage:10and50mg/kgAdministration:Intraperitonealinjection;10and50mg/kgonceResult:Tration-dependentlyinhibitedSer1292autophosphorylationwithanIC50of3nM.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?HumMolGenet.2017Jul15;26(14):2747-2767.?ProgramaOficialdeDoctoradoenBiomedicina.UniversidaddeGranada.5-Jul-2017.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].EstradaAA,etal.Discoveryofhighlypotent,selective,andbrain-penetrantaminopyrazoleleucine-richrepeatkinase2(LRRK2)small2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEmoleculeinhibitors.JMedChem.2014Feb13;57(3):921-36.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresea