A selective agonist of human TLR7
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Gardiquimod

Item No. 18877

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-amino-2-[(ethylamino)methyl]-α,α-dimethyl-1H-imidazo[4,5-c]quinoline-1-ethanol
CAS Number
1020412-43-4
Molecular Formula
C17H23N5O
Formula Weight
313.4
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 12 mg/mlPBS (pH 7.2): 0.2 mg/ml
λmax
249, 328 nm
SMILES
NC1=NC2=C(C3=C1N=C(CNCC)N3CC(C)(O)C)C=CC=C2
InChi Code
InChI=1S/C17H23N5O/c1-4-19-9-13-21-14-15(22(13)10-17(2,3)23)11-7-5-6-8-12(11)20-16(14)18/h5-8,19,23H,4,9-10H2,1-3H3,(H2,18,20)
InChi Key
FHJATBIERQTCTN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $54

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    10 mg

    $102

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    25 mg

    $185

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    50 mg

    $341

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    Cayman Chemical
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    Product Description

    Gardiquimod is an agonist of human toll-like receptor 7 (TLR7), but not human TLR8, although it activates both porcine TLR7 and TLR8.1 At 0.5 to 2 µg/ml, it enhances the immunosuppressive activity of T regulatory cells.2 Gardiquimod is effective as a mucosal adjuvant for Norwalk virus-like particles and inhibits infection of macrophages and T cells by HIV-1.3,4 It inhibits proliferation and migration while inducing apoptosis in pancreatic cancer cells in vitro.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhu, J., Lai, K., Bronile, R., et al. Porcine TLR8 and TLR7 are both activated by a selective TLR7 ligand, imiquimod. Mol. Immunol. 45(11), 3238-3243 (2008).

    2. Forward, N.A., Furlong, S.J., Yang, Y., et al. Signaling through TLR7 enhances the immunosuppressive activity of murine CD4+CD25+ T regulatory cells. J. Leukoc. Biol. 87(1), 117-125 (2010).

    3. Velasquez, L.S., Hjelm, B.E., Arntzen, C.J., et al. An intranasally delivered Toll-like receptor 7 agonist elicits robust systemic and mucosal responses to Norwalk virus-like particles. Clin. Vaccine Immunol. 17(12), 1850-1858 (2010).

    4. Buitendijk, M., Eszterhas, S.K., and Howell, A.L. Gardiquimod: A toll-like receptor-7 agonist that inhibits HIV type 1 infection of human macrophages and activated T cells. AIDS Res. Hum. Restroviruses 29(6), 907-918 (2013).

    5. Zou, B.B., Wang, F., Li, L., et al. Activation of Toll-like receptor 7 inhibits the proliferation and migration, and induces the apoptosis of pancreatic cancer cells. Mol. Med. Rep. 12(4), 6079-6085 (2015).