My cart
In the shopping cart is not goods, to choose and buy!
  • Product Name
  • Size
  • Quantity
  • Amount
    Selected items : 0 pieces Total : CHECK OUT()
    Vesatolimod (GS-9620)
    Vesatolimod (GS-9620)

    Price:
    Market Price:

    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V1860
    CAS #: 1228585-88-3Purity ≥98%

    Description: Vesatolimod (formerly known as GS-9620) is a novel potent, selective and orally bioactive small molecule agonist of Toll-like receptor 7 (TLR-7) with an EC50 of 291 nM. It has the potential for the treatment of chronic hepatitis B viral (HBV) infection. GS-9620 selectively induces IFN-α, cytokines and chemokines. The minimum effective concentrations for IFN-α induction were similar in pDCs and in PBMCs from HCV-positive donors. GS-9620 demonstrates an EC50 of 291 nM for human TLR7, which is 30-fold selectivity over TLR8 with EC50 of 9 μM. 

    References: Cardiol Rev. 2010 Sep-Oct;18(5):264-7; J Clin Invest. 2001 Jun;107(11):1423-32.

    Customer Validation
    Official Supplier of
    • VE
    • OF
    • YALE
    • hhmi
    • 香港大学
    Related Products
    Publications Citing InvivoChem Products
    • Citation of InvivoChem BMS-582949 (V2668)
    • Citation of InvivoChem Resveratrol (V0430)
    • Citation of InvivoChem venetoclax and S63845
    • Citation of InvivoChem KD025 (SLx-2119)
    • Citation of InvivoChem Tubastatin A HCl
    • Citation of InvivoChem BMS-1166
    • Physicochemical and Storage Information
    • Protocol
    • Quality Control Documentation
    • Related Biological Data
    • Customer Review
    Molecular Weight (MW)410.52 
    FormulaC22H30N6O2 
    CAS No.1228585-88-3 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: >4 mg/mL 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    SMILESO=C1NC2=C(N)N=C(OCCCC)N=C2N(CC3=CC=CC(CN4CCCC4)=C3)C1
    SynonymsGS-9620; GS 9620; GS9620 


    • Molarity Calculator
    • Dilution Calculator
    • The molarity calculator equation

      Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

      • Mass
      • Concentration
      • Volume
      • Molecular Weight *
      • =
      • ×
      • ×
    • The dilution calculator equation

      Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

      This equation is commonly abbreviated as: C1V1 = C2V2

      • Concentration (start)
      • ×
      • Volume (start)
      • =
      • Concentration (final)
      • ×
      • Volume (final)
      • ×
      • =
      • ×
      • C1
      •  
      • V1
      •  
      • C2
      •  
      • V2
    In Vitro

    In vitro activity: Vesatolimod (formerly known as GS-9620) is a novel potent, selective and orally bioactive small molecule agonist of Toll-like receptor 7 (TLR-7) with an EC50 of 291 nM. It has the potential for the treatment of chronic hepatitis B viral (HBV) infection. GS-9620 selectively induces IFN-α, cytokines and chemokines. The minimum effective concentrations for IFN-α induction were similar in pDCs and in PBMCs from HCV-positive donors. GS-9620 demonstrates an EC50 of 291 nM for human TLR7, which is 30-fold selectivity over TLR8 with EC50 of 9 μM. 


    Kinase Assay: 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.


    Cell Assay: Daudi cells are incubated for indicated times with varying concentrations [3H]Vesatolimod (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 Vesatolimod in cells is calculated from a calibration curve for Vesatolimod (GS-9620) mass versus radioactivity. Cell volume is measured.

    In VivoSingle 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 interferon-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) Cmax is 3.6±3.5, 36.8±34.5, and 55.4±81.0 nM, respectively. Peak serum interferon 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.
    Animal model Chimpanzees
    Formulation & Dosage 1 and 2 mg/kg; oral
    ReferencesGastroenterology. 2013 Feb 13. pii: S0016-5085(13)00169-8.PLoS One. 2016 Jan 19;11(1):e0146835.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    GS-9620


    GS-9620 rapidly distributes to and signals through the endo-lysosomal compartments.GS-9620

    Fig 3. Amino acid changes due to described single nucleotide polymorphisms (SNPs) do not impact GS-9620-dependent TLR7 activation.  2016 Jan 19;11(1):e0146835.

     GS-9620


    Structure-based mutational analysis identifies residues in TLR7 that are essential for GS-9620 in vitro activity.. From: Molecular Determinants of GS-9620-Dependent TLR7 Activation. 2016 Jan 19;11(1):e0146835.

     GS-9620


    GS-9620 induces phosphorylation of NF-κB and Akt in pDCs.

    GS-9620

    TLR7 dimers exist independent of GS-9620 binding.  2016 Jan 19;11(1):e0146835.


    评论

      Home Prev Next Last page / pices

      发评论

      ×
      Your information is safe with us. * Required Fields.
      Products are for research use only;  We do not sell to patients
      Tel: 1-708-310-1919
      Fax: 1-708-557-7486
      Subscribe to our E-newsletter
      • Name*
      • *
      • E-mail*
      • *
      • instructions:
      • *
      Copyright 2020 InvivoChem LLC | All Rights Reserved
      prompt
      Do you confirm the receipt?