Toll-like Receptor (TLR) Agonist

Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α.

Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid can directly trigger cancer cells to undergo apoptosis.

MC-Val-Cit-PAB-Amide-TLR7 agonist 4 formic (example 15) is a HER2-TLR7 and HER2-TLR8 immune agonist conjugate.

Polyinosinic-polycytidylic acid (Poly(I:C)) sodium is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis.

Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19.

ODN 1826 is a class B CpG ODN (oligodeoxynucleotide) and TLR9 agonist. ODN 1826 induces NO and iNOS production and enhances Apoptosis. ODN 1826 enhances immune surveillance. ODN 1826 increases aortic atherosclerotic plaque size. ODN 1826 has antitumor activity against lung cancer, glioma and melanoma.

Pam3CSK4 TFA is a toll-like receptor 1/2 (TLR1/2) agonist with an EC₅₀ of 0.47 ng/mL for human TLR1/2.

ODN 1826 sodium is a class B CpG ODN (oligodeoxynucleotide) and TLR9 agonist. ODN 1826 sodium induces NO and iNOS production and enhances Apoptosis. ODN 1826 sodium enhances immune surveillance. ODN 1826 sodium increases aortic atherosclerotic plaque size. ODN 1826 sodium has antitumor activity against lung cancer, glioma and melanoma.

Agatolimod sodium (ODN 2006) is a class B CpG ODN and is a TLR9 agonist. Agatolimod sodium can be used as vaccine adjuvant. Agatolimod sodium can be used for the research of cancer. Sequence: 5’-TCGTCGTTTTGTCGTTTTGTCGTT-3’.

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.

Zymosan A (Zymosan A from Saccharomyces cerevisiae) is a TLR2 agonist, that targeting TLRs can prevent and suppress IR-induced intestinal injury. Zymosan A exhibits a significant radioprotective effect, and protects IR-induced intestinal injury in mice. Zymosan A promotes the regeneration of intestinal stem cells (ISCs), after IR injury.

Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC₅₀=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC₅₀=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses.

ODN 2216 sodium is a type A CpG oligodeoxynucleotide vaccine adjuvant and a TLR9 agonist. ODN 2216 sodium interacts with TLR9 in the lysosomes of CD4⁺ T cells and activates feedback-dependent signaling pathways. ODN 2216 sodium induces the production of type I interferons, IL-6 and TGF-β via the IRAK4/IRF7 axis, while increasing intracellular ATP levels. ODN 2216 sodium not only induces the differentiation of CD4⁺ T cells into anti-inflammatory Th3-like regulatory phenotypes to inhibit autologous proliferation, but also enhances the specific CD8⁺ T cell-mediated cytotoxicity against Mammaglobin-A in breast cancer cells. ODN 2216 sodium is widely used in studies related to breast cancer and systemic lupus erythematosus.

Odetiglucan is a novel β-glucan that is a potent immunostimulant and a Dectin-1 (CLEC7A) agonist. Odetiglucan activates innate immune effector cells and triggers a coordinated anti-cancer immune response.

Imiquimod hydrochloride (R 837 hydrochloride), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod hydrochloride exhibits antiviral and antitumor effects in vivo. Imiquimod hydrochloride can be used for the research of external genital, perianal warts, cancer and COVID-19.

ODN 2216 is a type A CpG oligodeoxynucleotide vaccine adjuvant and a TLR9 agonist. ODN 2216 interacts with TLR9 in the lysosomes of CD4⁺ T cells and activates feedback-dependent signaling pathways. ODN 2216 induces the production of type I interferons, IL-6 and TGF-β via the IRAK4/IRF7 axis, while increasing intracellular ATP levels. ODN 2216 not only induces the differentiation of CD4⁺ T cells into anti-inflammatory Th3-like regulatory phenotypes to inhibit autologous proliferation, but also enhances the specific CD8⁺ T cell-mediated cytotoxicity against Mammaglobin-A in breast cancer cells. ODN 2216 is widely used in studies related to breast cancer and systemic lupus erythematosus.

ODN 1018 (1018 ISS) sodium is a TLR9 agonist and immune modulator. ODN 1018 sodium exhibits adjuvant activity and augments CD8+ T cell responses with LNP-encapsulated OVA peptides. ODN 1018 sodium triggers sustained suppression of allergic airway inflammation. ODN 1018 sodium can be used for the research of allergic asthma and systemic lupus erythematosus.

Motolimod (VTX-2337;VTX-378) is a selective Toll-like receptor 8 (TLR8) agonist, with an EC₅₀ of approximately 100 nM.

ODN 1018 (1018 ISS) is a TLR9 agonist and immune modulator. ODN 1018 exhibits adjuvant activity and augments CD8+ T cell responses with LNP-encapsulated OVA peptides. ODN 1018 triggers sustained suppression of allergic airway inflammation. ODN 1018 can be used for the research of allergic asthma and systemic lupus erythematosus.

Poly(I:C):Kanamycin (1:1) is a mixture of Poly(I:C) (HY-107202) and Kanamycin (HY-16566). Poly(I:C) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Poly(I:C) can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Poly(I:C) can directly trigger cancer cells to undergo apoptosis. Kanamycin stabilizes Poly(I:C).