TLR7
TLR7 is an endosomal pattern-recognition receptor that detects single-stranded RNA (ssRNA) and supports antiviral innate immunity[1]. Mechanistically, TLR7 activation engages IRF and NF-κB programs, producing type I interferon-related and inflammatory responses that vary by immune cell type[1]. In inflammatory contexts, NF-κB can also prime non-native TLR7-expressing cells to respond to TLR7 agonists with pro-inflammatory signaling[2]. Disease models link TLR7/TLR8 activation to lupus-related autoimmunity, and TLR7-driven signatures appear in human cells and lupus mouse models[1]. Compared with TLR8, TLR7 shows distinct ligand specificity, cellular expression, and pathway bias, supporting nonredundant functions among RNA-sensing endosomal isoforms[1][3]. In human monocytes during RNA virus infection, TLR7 and TLR8 activate distinct signaling pathways and generate different cytokine-related phenotypes[3]. For experimental applications, TLR7-selective agonists such as CL-087 help separate direct TLR7 responses from TLR8-driven inflammatory programs in human immune cells[1]. Small-molecule modulation remains useful for isoform-dissection studies because selective TLR8 antagonists demonstrate that closely related endosomal TLRs can be pharmacologically separated[4].
References:
- [1]. Bender AT, et al. TLR7 and TLR8 Differentially Activate the IRF and NF-κB Pathways in Specific Cell Types to Promote Inflammation. Immunohorizons. 2020 Feb 21;4(2):93-107. [Content Brief]
- [2]. Lee J, et al. Nuclear factor kappaB (NF-kappaB) activation primes cells to a pro-inflammatory polarized response to a Toll-like receptor 7 (TLR7) agonist. Biochem J. 2009 Jun 26;421(2):301-10. [Content Brief]
- [3]. de Marcken M, et al. TLR7 and TLR8 activate distinct pathways in monocytes during RNA virus infection. Sci Signal. 2019 Oct 29;12(605):eaaw1347. [Content Brief]
- [4]. Zhang S, et al. Small-molecule inhibition of TLR8 through stabilization of its resting state. Nat Chem Biol. 2018 Jan;14(1):58-64. [Content Brief]
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TLR7 Related Products (120)
Related Products (120)
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AYK004
0 ImagesCat. No.: HY-159916CAS No.: 3031612-90-2AYK004 is a TLR7/8 agonist that enhances immune responses by activating the TLR signaling pathway. AYK004 is an adenine derivative with a favorable hydrophilic-lipophilic balance, which improves the loading capacity and stability in immunoadjuvant systems such as liposomes, while reducing the side effects of the immunoadjuvant system in systemic immunity .
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FGT-4
0 ImagesCat. No.: HY-172934FGT-4 is a FR-β-targeted chimeric molecule. FGT-4 acts as a TLR7 agonist. FGT-4 binds to FR-β to enable delivery to tumor-associated macrophages and myeloid-derived suppressor cells. FGT-4 promotes the secretion of iNOS (associated with M1 macrophages) and the pro-inflammatory cytokine IL-6, and enhances the proliferation of cytotoxic CD8+ T cells. FGT-4 can be used for the research of breast cancer.
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3M-011
0 ImagesCat. No.: HY-121496CAS No.: 642473-62-93M-011 is a potent dual toll-like receptor TLR7/8 agonist and a cytokine inducer. 3M-011 significantly inhibits H3N2 influenza viral replication in the nasal cavity. 3M-011 is also a potent adjuvant to radiotherapy that induces local and profound systemic immune responses during radiotherapy. 3M-011 strongly has antitumor action.
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MTT5
0 ImagesCat. No.: HY-169017Purity: 98.49%MTT5 is a toll-like receptor 7 (TLR7) agonist. MTT5 can couple with Deruxtecan (HY-13631E) and exert anti-tumor activity in HER2 positive solid tumors through tumor cell killing and immune activation.
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SMU-L11-R
0 ImagesCat. No.: HY-179047CAS No.: 3040320-18-8SMU-L11-R is a selective TLR7 agonist with an EC50 of 0.012 μM for human TLR7. SMU-L11-R specifically activates TLR7, recruits MyD88, and triggers MAPK/NF-κB pathways, leading to TNF-α/IL-1β/IL-6 secretion in both mouse and human peripheral blood mononuclear cells. SMU-L11-R promotes M1-like macrophage polarization. SMU-L11-R exhibits excellent synergistic anti-tumor effects with PD-L1 inhibitors by upregulating CD8+T cells. SMU-L11-R shows potential in colorectal cancer studies.
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TLR7 agonist 8
0 ImagesCat. No.: HY-153073CAS No.: 2380231-81-0TLR7 agonist 8 is a TLR7 agonist with an EC50 of 0.12 nM for TLR7 and an EC50 of 0.76 nM for IL-6 induction. TLR7 agonist 8 can be used for research on diseases such as fibrosis, inflammatory diseases, cancer, or pathogen infections.
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ENDO12
0 ImagesCat. No.: HY-183079ENDO12 is an inhibitor of the Munc13-4-STX7 protein complex, with a Kd value of 2.7 µM for STX7. ENDO12 blocks the interaction of Munc13-4-STX7. ENDO12 inhibits endolysosomal flux, endolysosomal cargo degradation, the extracellular signal-regulated kinase signaling pathway in neutrophils, the IFN regulatory factor signaling pathway in plasmacytoid dendritic cells, and the responses of primary dendritic cells to TLR3, TLR7, and TLR9. ENDO12 alleviates CpG-induced systemic inflammation by reducing the levels of myeloperoxidase, IL-6 and IFNγ. ENDO12 does not interfere with the host's antiviral response to lymphocytic choriomeningitis virus infection.\nENDO12 can be used in studies related to systemic inflammation.
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TLR7/8 agonist 9
0 ImagesCat. No.: HY-153544CAS No.: 2649170-17-0TLR7/8 agonist 9 (Compound 25a) is a TLR7/8 agonist, with EC50s of 40 nM and 23 nM for hTLR7/8. TLR7/8 agonist 9 has anti-tumor activity and improves the antitumor activity of PD-1/PD-L1 blockade. TLR7/8 agonist 9 can be used for research of cancer immunotherapy.
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TLR7/8 antagonist 1
0 ImagesCat. No.: HY-145886CAS No.: 2901020-63-9TLR7/8 antagonist 1 (Compound 16c) is a competitive TLR7/8 antagonist with IC50 values of 3.91 μM and 2.19 μM, respectively. TLR7/8 antagonist 1 reduces agonist-induced production of proinflammatory cytokines, including TNFα, IFNγ and IL-1β.
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TLR7 agonist 26
0 ImagesCat. No.: HY-168157CAS No.: 1641544-09-3TLR7 agonist 26 (Compound 4) is a potent Toll-like receptor 7 (TLR7) agonist, with an EC50 of 225.5 nM. TLR7 agonist 26 shows immunopotentiating effects.
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AZ12441970
0 ImagesCat. No.: HY-117686CAS No.: 929551-91-7AZ12441970 is a potent and selectiveToll-like receptor 7 (TLR7) agonist, exhibiting pEC50s of 6.8 and 6.6 for human and rat TLR7. AZ12441970 shows efficacy in a mouse allergic airway model with minimal induction of systemic IFN-α. AZ12441970 can be used for allergic airway disease research.
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TLR7 agonist 14
0 ImagesCat. No.: HY-156175CAS No.: 2832199-45-6TLR7 agonist 14 (compound 17b) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 14 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations.
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BIM-46174
0 ImagesCat. No.: HY-183400CAS No.: 195450-11-4BIM-46174 is a heterotrimeric G protein complex inhibitor. BIM-46174 blocks GPCR downstream signaling by trapping Gα proteins in a nucleotide-free pocket conformation, thereby inhibiting Gαq-mediated calcium release, Gαs-mediated cAMP production, and GPCR-regulated cancer cell invasion. In vitro, BIM-46174 effectively suppresses a variety of clinically multidrug-resistant cell lines and induces tumor cell apoptosis through activation of caspase-3 and PARP cleavage. BIM-46174 also inhibits activation of the Neu1-MMP-9-GPCR signaling platform and downstream NF-κB signaling, and is widely used in the study of cancer signaling pathways and inflammation-related research, including lung cancer, pancreatic cancer, breast cancer, melanoma, and leukemia.
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UM-3006
0 ImagesCat. No.: HY-159919CAS No.: 1927013-87-3UM-3006 is a highly efficient TLR7/8 agonist that enhances immune responses by activating the TLR signaling pathway. UM-3006 holds significant research and application potential in the fields of vaccine adjuvants and immune diseases.
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BBIQ (GMP)
0 ImagesCat. No.: HY-111582GCAS No.: 1229024-57-0BBIQ (GMP) is BBIQ (HY-111582) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BBIQ is a potent and selectively toll-like receptor 7 (TLR7) agonist with an EC50 of 59.1 nM. BBIQ is a powerful vaccine adjuvant that enhances innate immune responses.
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Poly(U)
0 ImagesCat. No.: HY-131920CAS No.: 27416-86-0Synonyms: Polyuridylic acidPoly (U) (Polyuridylic acid) is an RNA chain that exists in a disordered extended state at room temperature and serves as a TLR7 ligand. Poly (U) produces distinguishable blocking effects when transported through α-hemolysin nanopores. Poly (U) forms a triple helix with adenosine or adenosine monophosphate, thereby significantly promoting the nucleotide bond condensation reaction between adenosine monophosphate and adenosine, while exerting minimal effects on other nucleosides. When conjugated with cationic lipids, Poly (U) specifically stimulates plasmacytoid dendritic cells to produce type I interferons.
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Enpatoran dihydrochloride
0 ImagesCat. No.: HY-134581BCAS No.: 2409589-21-3Synonyms: M5049 dihydrochlorideEnpatoran dihydrochloride (M5049 dihydrochloride) is an orally active and selective TLR7/8 antagonist. Enpatoran dihydrochloride inhibits the activation of the downstream type I interferon pathway. Enpatoran dihydrochloride is used in studies of cutaneous lupus erythematosus, systemic lupus erythematosus with cutaneous manifestations, and psoriasis.
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Creatine ethyl ester
0 ImagesCat. No.: HY-165632CAS No.: 15366-29-7Synonyms: CEE
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TLR7/8 agonist 13
0 ImagesCat. No.: HY-177300CAS No.: 1402802-45-2TLR7/8 agonist 13 is an orally active dual agonist of TLR7 (lowest effective concentrations (LEC) [hTLR7] = 1.6 μM) and TLR8 (LEC [hTLR8] = 1.6 μM). TLR7/8 agonist 13 exhibits agonistic activity against human peripheral blood mononuclear cells (hPBMCs) (LEC [hPBMC] = 0.5 μM). TLR7/8 agonist 13 induces endogenous IFNα, activating myeloid dendritic cells and monocytes toward a TH1 phenotype in mice and cynomolgus monkeys. TLR7/8 agonist 13 reduces viral load and HBV surface antigen expression in a mouse model of chronic AAV-HBV infection. TLR7/8 agonist 13 has the potential to indirectly induce IFNγ, which may promote HBV antigen-specific CD8 T cell-mediated responses. TLR7/8 agonist 13 can be used to study hepatitis B virus.
