A TLR7 and TLR8 agonist
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Telratolimod

Item No. 33172

Technical Information
Formal Name
N-[4-[(4-amino-2-butyl-1H-imidazo[4,5-c]quinolin-1-yl)oxy]butyl]-octadecanamide
CAS Number
1359993-59-1
Synonyms
  • MEDI9197
  • 3M-052
Molecular Formula
C36H59N5O2
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMSO: slightly solubleEthanol: slightly soluble
λmax
248 nm
SMILES
O=C(CCCCCCCCCCCCCCCCC)NCCCCON1C(CCCC)=NC2=C1C3=C(C=CC=C3)N=C2N
InChi Code
InChI=1S/C36H59N5O2/c1-3-5-7-8-9-10-11-12-13-14-15-16-17-18-19-27-33(42)38-28-22-23-29-43-41-32(26-6-4-2)40-34-35(41)30-24-20-21-25-31(30)39-36(34)37/h20-21,24-25H,3-19,22-23,26-29H2,1-2H3,(H2,37,39)(H,38,42)
InChi Key
RRTPWQXEERTRRK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Telratolimod is an agonist of toll-like receptor 7 (TLR7) and TLR8.1 It increases the production of IL-8 in HEK293 cells expressing human TLR7 or TLR8 and increases protein levels of IFN-α and TNF-α in isolated human peripheral blood mononuclear cells (PBMCs). Telratolimod (1 mg/kg) increases the HA-induced secretion of IFN-γ in mouse splenocytes ex vivo but does not induce the production of TNF-α in mouse serum in vivo. Telratolimod nanoparticles, when used as an adjuvant with the HIV-1 envelope glycoprotein, enhance neutralizing antibody responses to an HIV-1 pseudovirus in rhesus macaques for at least one year.2 Intratumoral administration of telratolimod reduces tumor growth and increases metastasis-free survival in E0771 and 4T1.2 murine mammary carcinoma models and increases intratumoral production of cytokines in a 4T1.2 murine model, an effect that is enhanced by coadministration of anti-PD-1 antibodies.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Smirnov, D., Schmidt, J.J., Capecchi, J.T., et alVaccine adjuvant activity of 3M-052: An imidazoquinoline designed for local activity without systemic cytokine induction. Vaccine 29(33), 5434-5442 (2011).

    2. Kasturi, S.P., Rasheed, M.A.U., Havenar-Doughton, C., et al3M-052, a synthetic TLR-7/8 agonist, induces durable HIV-1 envelope–specific plasma cells and humoral immunity in nonhuman primates. Sci. Immunol. 5(48), eabb1025 (2020).

    3. Zanker, D.J., Spurling, A.J., Brockwell, N.K., et alIntratumoral administration of the Toll-like receptor 7/8 agonist 3M-052 enhances interferon-driven tumor immunogenicity and suppresses metastatic spread in preclinical triple-negative breast cancer. Clin. Transl. Immunology 9(9), e1177 (2020).