Vesatolimod

SKU: orb1300412

Description

Vesatolimod

Research Area

Cell Biology, Immunology & Inflammation, Infectious Disease & Virology, Protein Biochemistry

Key Properties

• CAS Number: 1228585-88-3
• MW: 410.51
• Purity: 98.47%
• Formula: C₂₂H₃₀N₆O₂
• SMILES: CCCCOc1nc(N)c2NC(=O)CN(Cc3cccc(CN4CCCC4)c3)c2n1
• Target: HCV Protease,TLR,HBV,HIV Protease,Apoptosis
• Solubility: DMSO:4.11 mg/mL (10.01 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.44 mM)

Bioactivity

• Target IC50:
  TLR7:291 nM(EC50)
• In Vivo:
  Administering Single oral doses of GS-9620 at 0.3 and 1 mg/kg to uninfected chimpanzees resulted in a dose-dependent increase in serum interferon alpha (IFN-α), various cytokines/chemokines, and activation of interferon-stimulated genes (ISG) In both peripheral blood and liver tissues. Specifically, GS-9620 reached peak plasma concentration (Cmax) of 3. ± .5 nM at 0.3 mg/kg ( = ), 36. ± 4.5 nM at 1 mg/kg ( = ), and 55. ± 1.0 nM at 1 mg/kg ( = ), respectively with peak serum interferon responses recorded 8 hours after dosing the induced peak serum levels of IFN-α were measured at 66 pg mL fo the 0.3 mg/kg dose and 479 pg mL fo the 1 mg/kg dose. Treatment with GS-9620 at these doses also elevated ISG transcripts, specifically ISG15, OAS-1, MX1, IP-10 (CXCL10), and I-TAC (CXCL11), in peripheral blood mononuclear cells (PBMC) a the lower dose and In both PBMC and liver a the higher dose.
• In Vitro:
  Vesatolimod rapidly internalizes into cells and preferentially localizes to and signals from endo-lysosomal compartments. To test this hypothesis the kinetics of cellular uptake o the compound in Daudi cells using tritiated Vesatolimod (3H-Vesatolimod) is measured the kinetics of 3H-Vesatolimod accumulation is rapid, reaching concentration dependent steady-state equilibrium in approximately thirty minutes. Measured intracellular concentration of 3H-Vesatolimod is 5-fold higher tha the extracellular concentration of 3H-Vesatolimod used to treat cells. Increases in intracellular 3H-Vesatolimod concentration are roughly proportional with increasing concentration of 3H-Vesatolimo.
• Cell Research:
  GS-9620 is dissolved in DMSO and stored, and then diluted with appropriate medium before us. Daudi cells are incubated for indicated times with varying concentration [3H]GS-9620 (0.7μCi/mL). Cell associated radioactivity is extracted with ice cold 80% ethanol and measured using liquid scintillation counting the total amount of GS-9620 in cells is calculated from a calibration curve for GS-9620 mass versus radioactivity. Cell volume is measure.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

inhibit, Human immunodeficiency virus, Inhibitor, Hepatitis B virus, Hepatitis C virus, HBV, HCVProtease, HCV Protease, HCV, HIVProtease, HIV Protease, HIV, GS9620, GS-9620, GS 9620, Apoptosis, Vesatolimod, Toll-like Receptor (TLR), TLR7, TLR

Compound Identifiers

PubChem CID

46241268