Lanraplenib-GS-9876-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELanraplenibCat.No.:HY-109091CASNo.:1800046-95-0Synonyms:GS-9876分?式:C??H??N?O分?量:443.5作?靶點(diǎn):Syk作?通路:ProteinTyrosineKinase/RTK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:20mg/mL(45.10mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2548mL11.2740mL22.5479mL5mM0.4510mL2.2548mL4.5096mL10mM0.2255mL1.1274mL2.2548mL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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2mg/mL(4.51mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2mg/mL(4.51mM);ClearsolutionBIOLOGICALACTIVITY?物活性Lanraplenib(GS-9876)?種?度選擇性的?服SYK抑制劑(IC50=9.5nM)，?于研究炎癥性疾病。Lanraplenib(GS-9876)通過(guò)糖蛋?VI(GPVI)受體抑制??板中的SYK活性，?不會(huì)延長(zhǎng)猴?或?類的出?時(shí)間(BT)[1][2][3]。IC50&TargetIC50:9.5nM(SYK)[1]體外研究Lanraplenib(GS-9876)inhibitsanti-IgMstimulatedphosphorylationofAKT,BLNK,BTK,ERK,MEK,andPKCδinhumanBcellswithEC50valuesof24-51nM.Lanraplenib(GS-9876)inhibitsanti-IgMmediatedCD69andCD86expressiononB-cells(EC50=112±10nMand164±15nM,respectively)andanti-IgM/anti-CD40co-stimulatedBcellproliferation(EC50=108±55nM).Inhumanmacrophages,Lanraplenib(GS-9876)inhibitsIC-stimulatedTNFαandIL-1βrelease(EC50=121±77nMand9±17nM,respectively)[1].Lanraplenib(GS-9876)inhibitsglycoproteinVI(GPVI)-inducedphosphorylationoflinkerforactivationofTcellsandphospholipaseCγ2,plateletactivationandaggregationinhumanwholeblood,andplateletbindingtocollagenunderarterialflow[2].REFERENCES[1].DiPaoloJ,etal.FRI0049PreclinicalCharacterizationofGS-9876,ANovel,OralSYKInhibitorThatShowsEfficacyinMultipleEstablishedRatModelsofCollagen-InducedArthritis.AnnalsoftheRheumaticDiseases2016;75:443-444.[2].ClarkeAS,etal.EffectsofGS-9876,anovelspleentyrosinekinaseinhibitor,onplateletfunctionandsystemichemostasis.ThrombRes.2018Oct;170:109-118.[3].KivitzAJ,etal.GS-9876,aNovel,HighlySelective,SYKInhibitorinPatientswithActiveRheumatoidArthritis:Safety,TolerabilityandEfficacyResultsofaPhase2Study[abstract].ArthritisRheumatol.2018;70(suppl10).McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplic