Date published: 2025-11-21

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Gardiquimod (CAS 1020412-43-4)

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Alternate Names:
1-(4-Amino-2-ethylaminomethylimidazo[4,5-c]quinolin-1-yl)-2-methylpropan-2-ol
Application:
Gardiquimod is a TRL7 activator
CAS Number:
1020412-43-4
Purity:
≥98%
Molecular Weight:
313.40
Molecular Formula:
C17H23N5O
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Gardiquimod is a selective ligand for human or mouse toll-like receptor 7 (TLR7), which leads to the activation of NF-kappaB in HEK 293 cells expressing TLR7. At high concentrations (3 mug/ml), it slightly activates TLR8. Gardiquimod has more activity than imiquimod (sc-200385). By activating TLR7, gardiquimod stimulates the immune system to produce cytokines and other signaling molecules. Gardiquimod mimics the structure of certain nucleic acids, allowing it to bind to TLR7. Gardiquimod is extensively used in immunological research to study the activation and regulation of immune responses. It helps scientists understand how TLR7 signaling affects the behavior of various immune cells, including dendritic cells and B cells.


Gardiquimod (CAS 1020412-43-4) References

  1. Regioisomerism-dependent TLR7 agonism and antagonism in an imidazoquinoline.  |  Shukla, NM., et al. 2009. Bioorg Med Chem Lett. 19: 2211-4. PMID: 19285861
  2. The TLR7 agonists imiquimod and gardiquimod improve DC-based immunotherapy for melanoma in mice.  |  Ma, F., et al. 2010. Cell Mol Immunol. 7: 381-8. PMID: 20543857
  3. Dendritic cell activation and T cell priming with adjuvant- and antigen-loaded oxidation-sensitive polymersomes.  |  Scott, EA., et al. 2012. Biomaterials. 33: 6211-9. PMID: 22658634
  4. [Inhibitory effect of toll-like receptor 7 agonist on K562 cells].  |  Zhou, Y., et al. 2012. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 20: 579-82. PMID: 22739159
  5. Gardiquimod: a Toll-like receptor-7 agonist that inhibits HIV type 1 infection of human macrophages and activated T cells.  |  Buitendijk, M., et al. 2013. AIDS Res Hum Retroviruses. 29: 907-18. PMID: 23316755
  6. Induction of pro-inflammatory cytokine production in thymocytes by the immune response modifiers Imiquimod and Gardiquimod™.  |  Weber, A., et al. 2013. Int Immunopharmacol. 17: 427-31. PMID: 23867290
  7. Gardiquimod inhibits the expression of calcium-induced differentiation markers in HaCaT cells.  |  Jia, B., et al. 2013. Mol Biol Rep. 40: 6363-9. PMID: 24057248
  8. The activation of TLR7 regulates the expression of VEGF, TIMP1, MMP2, IL-6, and IL-15 in Hela cells.  |  Li, L., et al. 2014. Mol Cell Biochem. 389: 43-9. PMID: 24347177
  9. Activation of Toll-like receptor 7 inhibits the proliferation and migration, and induces the apoptosis of pancreatic cancer cells.  |  Zou, BB., et al. 2015. Mol Med Rep. 12: 6079-85. PMID: 26238718
  10. Combining vasculature disrupting agent and Toll-like receptor 7/8 agonist for cancer therapy.  |  Seth, A., et al. 2017. Oncotarget. 8: 5371-5381. PMID: 28036266
  11. Intraperitoneal gardiquimod protects against hepatotoxicity through inhibition of oxidative stress and inflammation in mice with sepsis.  |  Guo, S., et al. 2017. J Biochem Mol Toxicol. 31: PMID: 28422377
  12. Hybrid nanovaccine for the co-delivery of the mRNA antigen and adjuvant.  |  Yang, J., et al. 2019. Nanoscale. 11: 21782-21789. PMID: 31709434
  13. Adjuvant effects of TLR agonist gardiquimod admixed with Leishmania vaccine in mice model of visceral leishmaniasis.  |  Goyal, DK., et al. 2021. Infect Genet Evol. 93: 104947. PMID: 34052416
  14. Potential of TLR agonist as an adjuvant in Leishmania vaccine against visceral leishmaniasis in BALB/c mice.  |  Goyal, DK., et al. 2021. Microb Pathog. 158: 105021. PMID: 34089789
  15. Systemic toll-like receptor 9 agonist CpG oligodeoxynucleotides exacerbates aminoglycoside ototoxicity.  |  Yang, CH., et al. 2021. Hear Res. 411: 108368. PMID: 34678647

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Gardiquimod, 25 mg

sc-221663
25 mg
$154.00

Gardiquimod, 50 mg

sc-221663A
50 mg
$276.00

Gardiquimod, 100 mg

sc-221663B
100 mg
$506.00

Gardiquimod, 250 mg

sc-221663C
250 mg
$1154.00

Gardiquimod, 5 g

sc-221663D
5 g
$19743.00

Gardiquimod, 10 g

sc-221663E
10 g
$32136.00

Gardiquimod, 25 g

sc-221663F
25 g
$69366.00