Agatolimod  (Synonyms: ODN 2006; PF-3512676; CpG 7909; ODN 7909)

Agatolimod ((ODN 2006; PF-3512676; CpG 7909)) is a TLR9 agonist and immunomodulator with an EC₅₀ of 180 nM against human TLR9. Agatolimod activates and upregulates the expression of both TLR9 and TLR6, and mediates downstream signaling pathways via IRAK4, IRF5, IRF7. Agatolimod induces Th1-type innate and adaptive immune responses, activates various immune cells and promotes antigen presentation, regulates antibody levels and immune cell infiltration, upregulates the secretion of multiple cytokines, induces apoptosis and cell cycle arrest, enhances cytotoxicity, and clears intracellular Salmonella. Agatolimod is applicable to research on COVID-19, breast cancer, lung adenocarcinoma, HPV-related tumors, melanoma, and salmonellosis^{[1][2][3][4][5]}.

Agatolimod (10 μM) enhances expression of immunostimulatory cytokine IL-12p70 and chemoattractant cytokines in THP-1 cells, supporting its adjuvant activity^[2].
Agatolimod (10 μg/mL; 14 days) increases the radiosensitivity of R-A549 cells, as evidenced by a reduced D₀ value of 1.33 Gy in clonogenic assays when combined with radiation^[3].
Agatolimod stimulates TLR9 signaling in HEK-Blue-hTLR9 cells with an EC₅₀ of 180 nM^[4].
Agatolimod (1-6 μM; 24 h) increases K55 cell surface marker expression in HD11 chicken macrophage cells in a dose-dependent manner (1-3 μM) but does not affect MHC class I or II expression^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Agatolimod sodium (1-50 μg/injection; i.m.; twice at a 2-week interval) adjuvant enhances anti-spike IgG and neutralizing antibody titers in an antigen dose-dependent manner, reduces eosinophilic lung infiltration, and results in 100% survival (consistent with S-protein antigen alone) following SARS-CoV-2 challenge^[1].
Agatolimod (5 nmol; s.c.; days 7 and 14 after tumor inoculation) enhances the anti-tumor effect of the TRP2 peptide vaccine against TRP2-expressing B16F10 melanoma in mice, though less potently than S-540956^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

7699.00

525625-52-9

Solid

White to off-white

DNA, d(P-thio)(T-C-G-T-C-G-T-T-T-T-G-T-C-G-T-T-T-T-G-T-C-G-T-T)

[Agatolimod]

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [1]. Sonoyama T, et al. Results from a preclinical study in rodents and a Phase 1/2, randomized, double-blind, placebo-controlled, parallel-group study of COVID-19 vaccine S-268019-a in Japanese adults. Vaccine. 2023;41(11):1834-1847.  [Content Brief]

  [2]. Babaer D, et al. Oligodeoxynucleotides ODN 2006 and M362 Exert Potent Adjuvant Effect through TLR-9/-6 Synergy to Exaggerate Mammaglobin-A Peptide Specific Cytotoxic CD8+T Lymphocyte Responses against Breast Cancer Cells. Cancers (Basel). 2019;11(5):672. Published 2019 May 14.  [Content Brief]

  [3]. Yan L, et al. CpG-ODN 7909 increases radiation sensitivity of radiation-resistant human lung adenocarcinoma cell line by overexpression of Toll-like receptor 9. Cancer Biother Radiopharm. 2013;28(7):559-564.  [Content Brief]

  [4]. Nakagawa T, et al. S-540956, a CpG Oligonucleotide Annealed to a Complementary Strand With an Amphiphilic Chain Unit, Acts as a Potent Cancer Vaccine Adjuvant by Targeting Draining Lymph Nodes. Front Immunol. 2021;12:803090. Published 2021 Dec 23.  [Content Brief]

  [5]. Xie H, et al. CpG-induced immunomodulation and intracellular bacterial killing in a chicken macrophage cell line. Dev Comp Immunol. 2003;27(9):823-834.  [Content Brief]