tlr7

TLR7/8 agonist 7, a compound that functions as a TLR7/8 agonist, plays a pivotal role in activating various immune cells and is instrumental in the synthesis of immune-stimulating antibody conjugate (ISAC) molecules. This compound holds significant potential for research in immunology.

TLR7/8-IN-1, a crystalline TLR7/TLR8 inhibitor, is a valuable compound for autoimmune disease research[1].

TLR7/8/9 antagonist 2 is an orally active and highly bioavailable vTLR7/8/9 antagonist. TLR7/8/9 antagonist 2 inhibits HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC50s of 0.011 μM, 0.029 μM and 0,052 μM, respectively. TLR7/8/9 antagonist 2 can be used to study auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis.

TLR7 agonist 2 (TLR7-IN-1) is a specific and effective Toll-like Receptor 7 (TLR7) agonist (LEC=0.4 μM).

TLR7/8 agonist 4 hydroxy-PEG6-acid, a Drug-Linker Conjugate for ADCs, comprises the TLR7/8 agonist 4 and a hydroxy-PEG6-acid linker, suitable for the synthesis of antibody-drug conjugates (ADCs) [1].

TLR7/8 agonist 9 (Compound 25a), exhibiting EC50 values of 40 nM and 23 nM for hTLR7 and hTLR8 respectively, demonstrates anti-tumor properties and enhances the efficacy of PD-1/PD-L1 blockade treatments. This compound is utilized in cancer immunotherapy research [1].

Compound 17b, a TLR7 agonist also known as TLR7 agonist 14, exhibits high potency with an EC50 of 18 nM. It effectively activates mouse macrophages and human peripheral blood mononuclear cells (hPBMCs) at low-nanomolar concentrations [1].

TLR7/8 agonist 4 (compound 41) is a potent agonist of TLR7/8 with anti-cancer activity [1].

TLR7/8 agonist-7d is a useful organic compound for research related to life sciences and the catalog number is T64606.

TLR7 agonist 12 (example 20), a purine nucleoside analog, functions as a TLR7 agonist with broad antitumor activity, particularly against indolent lymphoid malignancies. Its anticancer mechanisms include DNA synthesis inhibition, apoptosis induction, among others [1] [2].

TLR7/8 agonist 4 hydroxy-PEG10-acid (compound 9) is a drug-linker conjugate employed in antibody-drug conjugates (ADC). This compound exhibits remarkable antitumor activity by utilizing TLR7/8 agonist 4, which acts as a potent activator of TLR7/8. The TLR7/8 agonist 4 is linked to hydroxy-PEG10-acid, the ADC linker, via a cleavable bond. Overall, it demonstrates promising pharmaceutical potential in the context of ADC-based therapeutics.

TLR7/8/9-IN-1 is a potent inhibitor of Toll-like receptors 7/8/9 (TLR7/8/9) with an IC50 of 43 nM.

TLR7/8 agonist 1 is a toll-like receptor ( TLR7 )/ TLR8 dual-agonistic imidazoquinoline.

TLR7/8 agonist 4 TFA (compound 41) is a highly potent TLR7/8 agonist that exhibits significant anti-cancer activity.

TLR7 agonist 15 (compound 16b) is a potent activator of mouse macrophages and hPBMCs, demonstrating an EC50 of 18 nM. It induces robust responses at low-nanomolar concentrations [1].

TLR7/8 agonist 4 hydroxy-PEG6-acid hydrochloride, a Drug-Linker Conjugate for ADC synthesis, is the hydrochloride variant of TLR7/8 agonist 4 hydroxy-PEG6-acid, comprising the TLR7/8 agonist 4 component attached to the hydroxy-PEG6-acid linker [1].

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

TLR7 agonist 4 (Compound 1.2) is a TLR7 agonist (EC50: 4.3 nM).

TLR7 agonist 10 is a Nucleoside Derivative - Xylo-nucleoside, N-Methylated alkylated nucleoside; 8-Modified purine nucleoside.

TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride (compound 9) is a drug-linker conjugate used in antibody-drug conjugates (ADCs) with high efficacy against tumors. It consists of TLR7/8 agonist 4, a potent TLR7/8 agonist, linked to the ADC linker hydroxy-PEG10-acid which can be cleaved.

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

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

TLR7 agonist 3 (Compound 2), a potent activator of toll-like receptor 7 (TLR7), plays a critical role in initiating immune responses, positioning it as a promising target for immunomodulator development.

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 has been shown to enhance the efficacy of PD-1/PD-L1 inhibitors in antitumor activity [1].

TLR7 agonist 16 (compound 16d) is a potent activator of TLR7 with an EC50 value of 18 nM. It effectively triggers the activation of both mouse macrophages and human peripheral blood mononuclear cells (hPBMCs) at low-nanomolar levels [1].

TLR7 agonist 13 is a useful organic compound for research related to life sciences. The catalog number is TNU1350 and the CAS number is 2389988-70-7.

TLR7 agonist 1 is a selective and oral TLR7 agonist (IC50: 90 nM).

TLR7/8 antagonist 2 (Compound 15) is a highly potent and orally active agonist of TLR7/8, exhibiting IC50 values of 4.9 and 0.6 nM for TLR7 and TLR8, respectively. Its strong affinity for these receptors makes it a promising candidate for the treatment and investigation of autoimmune diseases, including lupus erythematosus, which is associated with inappropriate activation of TLR7 and TLR8. Consequently, TLR7/8 antagonist 2 represents a valuable tool for research in the field of autoimmune diseases [1].

MC-Val-Cit-PAB-Amide-TLR7 agonist 4 (example 15) is a conjugate that acts as an immune agonist targeting both HER2-TLR7 and HER2-TLR8 pathways [1].

TLR7/8 Antagonist 1 (Compound 16c), an imidazoquinoline derivative, is a potent TLR7/8 agonist with IC50 values of 3.91 and 2.19 μM for TLR7 and TLR8, respectively. rel-O-2050 (TLR-2050) is a key target for drug development in infectious diseases, cancer and autoimmune diseases.

1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects.

Hydroxychloroquine (2-[[4-[(7-Chloroquinolin-4-yl)amino]pentyl](ethyl)amino]ethanol) (HCQ) is an alkalinizing lysosomatropic drug that acts by inducing apoptosis of renal cancer cells in vitro and inhibiting TLR7/9. It is a medication used to prevent and treat malaria, and it's also being studied as an experimental treatment for COVID-19.

DSR-6434 is a selective agonist of TLR7 with antitumor effect. DSR-6434 exhibits EC50s of 7.2 nM and 4.6 nM for human and mouse.

Isatoribine(ANA245) free base is a potent TLR7 receptor agonist with anti-hepatitis C virus infection activity for the study of HCV infection.

AZD8848 is a selective antedrug agonist of toll-like receptor 7 (TLR7). It is developed for the research of asthma and allergic rhinitis.

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.

CL264, a selective agonist of TLR7, can be used in studies about innate immune signals.

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.

Resiquimod (R848) is an imidazoquinoline amine and Toll-like receptor (TLR) agonist with potential immune response modifying activity. Resiquimod exerts its effect through the TLR signaling pathway by binding to and activating TLR7 and 8 mainly on dendritic cells, macrophages, and B-lymphocytes. This induces the nuclear translocation of the transcription activator NF-kB as well as activation of other transcription factors. This may lead to an increase in mRNA levels and subsequent production of cytokines, especially interferon-alpha (INF-a) and other cytokines, thereby enhancing T-helper 1 (Th1) immune responses. In addition, topical application of resiquimod appears to activate Langerhans' cells, leading to an enhanced activation of T-lymphocytes.

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

E104 (compound 1), a selective TLR7 agonist, exhibits potent anticancer activity when delivered via antibody-drug conjugate (ADC) technology. It effectively activates mouse macrophages and human peripheral blood mononuclear cells (hPBMCs) [1].

Guretolimod is a Toll-like receptor 7 (TLR7) agonist.

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.

Imiquimod 2HCl is a toll-like receptor 7 (TLR7) agonist and an immunomodulator with antiviral and antitumor activity.Imiquimod 2HCl can be used to construct a psoriasis-like mouse model, which can be used to study periocular skin cancers, pemphigus foliaceus, and COVID-19 infection.

SM-276001 is a potent selective agonist of TLR7,and is an orally active interferon (IFN) inducer.

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.

Gardiquimod diTFA, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod diTFA could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 when used at concentrations below 10 μM. Gardiquimod diTFA could function as both an immune system modifier and a reverse transcriptase inhibitor as a novel therapeutic agent to block systemic and mucosal transmission of HIV-1.[1] [2].

GSK2245035 is a highly selective intranasal TLR7 agonist with preferential Type-1 interferon (IFN)-stimulating properties (pEC50s: 9.3 and 6.5 for IFNα and TFNα). It effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood

Vesatolimod (GS-9620) is an effective and specific orally active agonist of Toll-like receptor 7.

ODN 105870, a G-modified inhibitory oligonucleotide (INH-ODN), selectively inhibits TLR7 and is utilized in the research of inflammatory immune responses [1].

(S)-Hydroxychloroquine is the enantiomer of Hydroxychloroquine. Hydroxychloroquine shows efficiently inhibits SARS-CoV-2 infection in vitro.

(R)-Hydroxychloroquine is the enantiomer of Hydroxychloroquine. Hydroxychloroquine is an agent of synthetic antimalarial.

Hydroxychloroquine sulfate (Acidum iopanoicum) inhibits plasmodial heme polymerase. It is a chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa.