tlr7/tlr8

CU-115 is a selective and potent TLR8 antagonist with IC50 of 1.04 µM and =>50 µM for TLR8 and TLR7, respectively. CU-115 decreases production of TNF-α and IL-1β activated by R-848 in THP-1 cells.

Enpatoran is an inhibitor of TLR7(IC50 = 11.1 nM) and TLR8(IC50 = 24.1 nM). Enpatoran was found to be inactive against TLR3, TLR4, and TLR9 in vitro and in vivo.

Imiquimod (R 837) is an immune response modifier that acts as a toll-like receptor 7 agonist.

Resiquimod (R848) is a Toll-like receptor 7 8 (TLR7 TLR8) agonist that induces cytokine upregulation. Resiquimod is an immunomodulator with antitumor and antiviral activity.

MC-Val-Cit-PAB-Amide-TLR7 agonist 4 TFA is the trifluoroacetate form of MC-Val-Cit-PAB-Amide-TLR7 agonist 4. MC-Val-Cit-PAB-Amide-TLR7 agonist 4 is a HER2-TLR7 and HER2- TLR8 immune agonist complexes with potential antitumor activity by activating the TLR7 and TLR8 signaling pathways and enhancing immune responses.

Motolimod (VTX-378) (VTX-2337) is an effective and specific Toll-like receptor (TLR) 8 agonist (EC50: 100 nM), > 50-fold selectivity over TLR7.

TLR7 8 agonist 3 is a potent activator of TLR7 and TLR8.

AXC-715 trihydrochloride (T785 trihydrochloride) is a TLR7 TLR8 dual agonist for the synthesis of antibody-adjuvanted immunocouplings. The couplings are mostly programmed death ligand 1 (PD-L1) attached to one or more antibody structures of the adjuvant.

BMS-905 is a potent dual inhibitors of TLR7 and TLR8 with good selectivity against TLR9 and other family members. BMS-905 can be used in studies about the treatment of diseases such as psoriasis, arthritis, and lupus.

TLR7 8 agonist 1 is a toll-like receptor TLR7 TLR8 agonist with anticancer and antiviral activities and can be used to study immune-related diseases.

Gardiquimod is a TLR7 8 agonist. When used at concentrations below 10 μM, Gardiquimod specifically activates TLR7. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells.

CL097 hydrochloride is a potent TLR7 and TLR8 agonist. CL097 hydrochloride induces pro-inflammatory cytokines in macrophages and NADPH oxidase priming, thereby increasing the fMLF-stimulated ROS production [2].

TLR7 8 agonist 1 dihydrochloride (TLR7 8 agonist-5d) is a TLR7 8 agonist which shows prominent immunostimulatory activities.

PVP-037 is an effective adjuvant and agonist for TLR7 and TLR8, demonstrating broad innate immune activation and enhancing vaccine immune responses.

AXC-715 hydrochloride is a TLR7/TLR8 dual agonist, can be used for synthesis of antibody-adjuvant immunoconjugates, comprising an antibody construct that binds programmed death-ligand 1 (PD-L1) linked to one or more adjuvants.

Telratolimod (MEDI9197) is a toll-like receptors 7 8 agonist. It has an antitumor activity.

TLR7 8 agonist 8 (compound 24m) is a potent dual agonist for toll-like receptors 7 and 8 (TLR7 8), exhibiting half-maximal effective concentrations (EC50s) of 27 nM for human TLR7 (hTLR7) and 12 nM for human TLR8 (hTLR8). This compound enhances the efficacy of PD-1 PD-L1 inhibitors in antitumor activity [1].

CL097 is an effective agonist of TLR7 and TLR8. CL097 induces pro-inflammatory cytokines in macrophages and NADPH oxidase priming, thereby increasing the fMLF-stimulated ROS production.

TLR8 agonist 2 hydrochloride is a highly potent and selective agonist for human TLR8, with an EC50 of 3 nM, but demonstrates significantly weaker activity towards human TLR7 (EC50 of 33.33 μM).

m-AM-BBIQ (compound 10) is a dual agonist for TLR7 and TLR8, exhibiting EC50 values of 0.12 μM and 1.7 μM for hTLR7 and hTLR8, respectively.

TLR7 agonist20 hydrochloride is an imidazoquinoline analog that functions as a potent and specific agonist for TLR7, with an EC50 value of 0.23 μM against hTLR7. It demonstrates strong adjuvant activity in enhancing spike antibody levels and induces a robust T helper cell 1 (Th1) response. Additionally, it increases levels of IgG2b and IgG2c, aside from IgG1.

3M-011, a potent dual toll-like receptor TLR7 8 agonist and cytokine inducer, serves as a powerful adjuvant to radiotherapy, eliciting significant local and systemic immune responses. Additionally, it effectively inhibits H3N2 influenza viral replication in the nasal cavity and exhibits strong antitumor activity[1][2][3].

TLR7 8 agonist 6 (Compound 4), an imidazoquinoline derivative, is a potent TLR7 8 agonist with IC50 values of 0.18 μM for TLR7 and 5.34 μM for TLR8 [TLR7 8 Antagonist].