Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESelgantolimodCat.No.:HY-109137CASNo.:2004677-13-6Synonyms:GS-9688分?式:C??H??FN?O分?量:293.34作?靶點(diǎn):Toll-likeReceptor(TLR);HBV作?通路:Immunology/Inflammation;Anti-infection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:62.5mg/mL(213.06mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.4090mL17.0451mL34.0901mL5mM0.6818mL3.4090mL6.8180mL10mM0.3409mL1.7045mL3.4090mL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:≥2.5mg/mL(8.52mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.52mM);ClearsolutionBIOLOGICALACTIVITY?物活性Selgantolimod(GS-9688)?種?服活性，有效和選擇性的Toll樣受體8(TLR8)激動(dòng)劑，?于?型肝炎病毒(HBV)和HIV感染的研究。IC50&TargetTLR8HBV體外研究Selgantolimodinducesthecellularimmunemediatorsinterleukin(IL)-12andIL-8,aswellastheantiviralcytokinestumornecrosisfactor-αandIFN-γinvitroinhumanperpheralbloodmononuclearcells[1].Selgantolimodactivatesnaturalkiller(NK)andmucosalassociatedinvariantTcells,stimulatesclusterofdifferentiation(CD)-8+T-cellproliferation,andincreasIFNγproduction,whileloweringprogrammedcelldeathprotein1expressionbyHBV-specificCD8+-Tcellsinvitroinperipheralbloodmononuclearcells[1].Selgantolimod-inducedcytokinesreduceHBVDNA,RNA,andantigenlevelsinHBV-infectedprimaryhumanhepatocytes[1].體內(nèi)研究Once-weeklydosingoforalSelgantolimodinducesdose-dependentincreasesinserumIL-12andIL-1receptorantagonist(IL-1RA)incynomolgusmonkeys,andleadstofunctionalcureinthewoodchuckmodelofchronicHBV[1].REFERENCES[1].JulesLevin.EfficacyandSafetyofOralTLR8AgonistSelgantolimodinVirallySuppressedAdultPatientsWithChronicHepatitisB:aPhase2,Randomized,Double-Blind,Placebo-Controlled,MulticenterStudy.2019Nov8-12.[2].BenjaminRyan.SelgantolimodShowsPromiseasTreatmentforHepatitisB.November18,2019.[3].RomasGeleziunas,etal.Modulatorsoftoll-likereceptorsforthetreatmentofhiv.US20170071944A1.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications