Vesatolimod维沙莫德,1228585-88-3

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Vesatolimod

CAS No. : 1228585-88-3

MCE 国际站：Vesatolimod

产品活性：Vesatolimod (GS-9620) 是一种有效，选择性，可口服的 Toll 样受体7 (TLR7) 激动剂，EC₅₀ 值为291 nM。

研究领域：Immunology/Inflammation  |  Apoptosis  |  Anti-infection

作用靶点：Toll-like Receptor (TLR)  |  Apoptosis  |  HBV  |  HCV  |  HIV

In Vitro: Vesatolimod (GS-9620) rapidly internalizes into cells and preferentially localizes to and signals from endo-lysosomal compartments. To test this hypothesis, the kinetics of cellular uptake of the compound in Daudi cells using tritiated Vesatolimod (³H-GS-9620) is measured. The kinetics of ³H-GS-9620 accumulation is rapid, reaching concentration-dependent steady-state equilibrium in approximately thirty minutes. Measured intracellular concentration of ³H-Vesatolimod is 5-fold higher than the extracellular concentration of ³H-GS-9620 used to treat cells. Increases in intracellular ³H-Vesatolimod concentrations are roughly proportional with increasing concentrations of ³H-GS-9620.

In Vivo: Single oral doses of Vesatolimod (GS-9620) at 0.3 and 1 mg/kg in uninfected chimpanzees demonstrates a dose- and exposure-related induction of serum IFN-α, select cytokines/chemokines, and IFN-stimulated genes (ISG) in the peripheral blood and liver. Following oral administration at 0.3 (n=3), and 1 mg/kg (n=3 and n=4), Vesatolimod (GS-9620) C_max is 3.6±3.5, 36.8±34.5, and 55.4±81.0 nM, respectively. Peak serum IFN responses occur at 8 h post-dose. The mean peak levels of induced serum IFN-α are 66 and 479 pg/mL at doses of 0.3 and 1 mg/kg, respectively. Vesatolimod (GS-9620) treatment induces ISG transcripts including ISG15, OAS-1, MX1, IP-10 (CXCL10), and I-TAC (CXCL11) in peripheral blood mononuclear cells (PBMC) at 0.3 mg/kg and in both PBMC and the liver at 1 mg/kg.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Anti-Infection Compound Library  |  Apoptosis Compound Library  |  Immunology/Inflammation Compound Library  |  Clinical Compound Library  |  Antiviral Compound Library  |  Small Molecule Immuno-Oncology Compound Library  |  Drug Repurposing Compound Library  |  Antioxidant Compound Library  |  Reprogramming Compound Library  |  Oxygen Sensing Compound Library  |  Pyroptosis Compound Library  |  Orally Active Compound Library  |  Anti-Hepatitis C Virus Compound Library  |  Human Metabolite Library  |  Heterocyclic Compound Library  |  Pain-Related Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  Autoimmune Disease Compound Library  |  Highly Selective Inhibitors Library  |  Highly Selective Activators Library  |  Cytokine Inhibitors Library  |  Cell Death Library  |  MG-132  |  Chloroquine  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  LY294002  |  Tamoxifen  |  Paclitaxel  |  Lipopolysaccharides  |  Y-27632  |  Acetylcysteine  |  Angiotensin II human  |  2-Deoxy-D-glucose  |  Staurosporine  |  SB-431542  |  Actinomycin D  |  Deferoxamine mesylate  |  Bortezomib  |  5-Fluorouracil  |  Trametinib  |  Sorafenib  |  Oxaliplatin  |  Gemcitabine  |  Temozolomide  |  Rotenone  |  Mdivi-1  |  Elesclomol  |  Ruxolitinib  |  Decitabine  |  SP600125  |  MK-2206 dihydrochloride

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds