Selgantolimod-GS-9688-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESelgantolimodCat.No.:HY-109137CASNo.:2004677-13-6Synonyms:GS-9688分⼦式:C₁₄H₂₀FN₅O分⼦量:293.34作⽤靶点:Toll-likeReceptor(TLR);HBV作⽤通路:Immunology/Inflammation;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:62.5mg/mL(213.06mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.4090mL17.0451mL34.0901mL5mM0.6818mL3.4090mL6.8180mL10mM0.3409mL1.7045mL3.4090mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(8.52mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.52mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Selgantolimod(GS-9688)⼀种⼝服活性，有效和选择性的Toll样受体8(TLR8)激动剂，⽤于⼄型肝炎病毒(HBV)和HIV感染的研究。IC50&TargetTLR8HBV体外研究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].体内研究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