Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGSK963Cat.No.:HY-103028ACASNo.:2049868-46-2分?式:C??H??N?O分?量:230.31作?靶點(diǎn):RIPkinase作?通路:Apoptosis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:25mg/mL(108.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM4.3420mL21.7099mL43.4197mL5mM0.8684mL4.3420mL8.6839mL10mM0.4342mL2.1710mL4.3420mL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:2.5mg/mL(10.85mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(10.85mM);ClearsolutionBIOLOGICALACTIVITY?物活性GSK963?種?性的、強(qiáng)效的、選擇性的受體相互作?蛋?1(RIP1)酶的抑制劑，其IC50值為29nM。GSK963對(duì)體外??和?細(xì)胞的壞死具有強(qiáng)效和選擇性的抑制作?。IC50&TargetIC50:29nM(RIP1inFPbindingassay)[1].體外研究GSK963is>10?000-foldselectiveforRIP1over339otherkinases,lacksmeasurableactivityagainstIDOandhasaninactiveenantiomer,GSK962,whichcanbeusedtoconfirmon-targeteffects[1].體內(nèi)研究GSK963(2mg/kg)resultsinacompleteprotectionfromTNF+zVAD-inducedtemperatureloss.GSK963(0.2?mg/kg)alsoshowsasignificantresponse[1].AnimalModel:C57BL/6mice[1].Dosage:0.2mg/kg,2mg/kg,10?mg/kg.Administration:IPonce.Result:ProtectedmicefromTNF+zVAD-inducedhypothermia.REFERENCES[1].BergerSB,etal.CharacterizationofGSK'963:astructurallydistinct,potentandselectiveinhibitorofRIP1kinase.CellDeathDiscov.2015Jul27;1:15009.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-8