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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TLR7 agonist 28
0 ImagesCat. No.: HY-170899CAS No.: 1801518-98-8TLR7 agonist 28 (compound 3) is a potent TLR7 agonist. TLR7 agonist 28 can conjugat to antitumor monoclonal antibodies (mAbs) for cancer immunotherapy.
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TLR7 agonist 29
0 ImagesCat. No.: HY-173070CAS No.: 2275612-76-3TLR7 agonist 29 (Compound 1) is the agonist for TLR7 with an EC50 of 5.2 nM for human TLR7 (EC50 for mouse TLR7 is 48.2 nM). TLR7 agonist 29 activates bone marrow-derived macrophages (BMDMs), stimulates myeloid cells in the tumor microenvironment, promotes the expression of PD-L1, CD86 and IFN-α. TLR7 agonist 29 can be used as payload for synthesis of ADC.
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TLR7/8/9 antagonist-3
0 ImagesCat. No.: HY-187531CAS No.: 2403782-38-5TLR7/8/9 antagonist-3 is an orally active antagonist of TLR7, TLR8 and TLR9, with human IC50 values of 0.008 μM, 0.006 μM and 0.072 μM, respectively. TLR7/8/9 antagonist-3 blocks agonist-induced activation of hTLR7, hTLR8, hTLR9, mTLR7 and mTLR9, and reduces serum IFNα and TNFα levels. TLR7/8/9 antagonist-3 can be used in the research of autoimmune diseases.
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TLR7 agonist 7
0 ImagesCat. No.: HY-153072CAS No.: 2380231-77-4TLR7 agonist 7 (compound IIb-26) is an TLR7 agonist with an EC50 value of ~4 nM.
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SMU-R39
0 ImagesCat. No.: HY-175782SMU-R39 is a TLR7 and TLR8 antagonist with IC50 values of 3.22 μM and 0.24 μM, respectively. SMU-R39 binds to recombinant mTLR7 protein (KD = 2.36 μM) and to recombinant hTLR8 protein (KD = 105 nM). SMU-R39 suppresses downstream NF-κB and MAPK signaling, and reduces secretion/transcription of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in PBMCs and THP-1 cells. SMU-R39 demonstrates anti-inflammatory efficacy in Imiquimod (IMQ) (HY-B0180)-induced psoriasis mouse model. SMU-R39 can be used for the study of autoimmune diseases such as psoriasis.
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TLR7 agonist 21
0 ImagesCat. No.: HY-163670CAS No.: 3040038-00-1TLR7 agonist 21 (Compound 27B) is a selective agonist for Toll-like receptor 7(TLR7), with an EC50 of 17.53 nM (for human TLR7) and 41.7 nM (for mouse TLR7). TLR7 agonist 21 stimulates the secretion of pro-inflammatory cytokines, such as IL-6, TNF-α, IFN-α1, and IL-4. TLR7 agonist 21 acts as a vaccine adjuvant, increases levels of IgG and IgA, and protects the mouse from influenza virus infections.
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TLR7 agonist 24
0 ImagesCat. No.: HY-162725TLR7 agonist 24 (Compound 21) is an agonist for TLR7 with EC50 of 3.72 μM. TLR7 agonist 24 can be used as a vaccine adjuvant when combined with Aluminum Hydroxide (HY-B1521), that enhances the immune response against SARS-CoV-2 and hepatitis B antigens.
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AYK004-B1
0 ImagesCat. No.: HY-159914CAS No.: 3031612-91-3AYK004-B1 is a TLR7 agonist (EC50=0.2265 nM). AYK004-B1 can be used to prepare immune adjuvants.
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TLR7/8 agonist 14
0 ImagesCat. No.: HY-179336TLR7/8 agonist 14 is a TLR7 and TLR8 agonist with EC50 values of 0.53 μM and 4.3 μM, respectively. TLR7/8 agonist 14 increases the secretion of the proinflammatory cytokines TNF-α, IL-1β, IL-8 and IFN-γ. TLR7/8 agonist 14 increases cytokine secretion and expression of CD86. LR7/8 agonist 14 can be used for research colorectal carcinoma.
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TLR7 agonist 9
0 ImagesCat. No.: HY-152726CAS No.: 2389988-38-7TLR7 agonist 9 (compound 10) is an aonist of TLR7. TLR7 agonist 9 can be used for research of cancer and infectious disease. TLR7 agonist 9 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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ETI60
0 ImagesETI60 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.68 μM) and TLR9 (IC50 = 0.12 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI60 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI60 modulates the expression of genes associated with inflammation. ETI60 effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI60 can be used for autoimmune and inflammatory diseases research.
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TLR7 agonist 27
0 ImagesCat. No.: HY-168159TLR7 agonist 27 (compound 24) is a potent TLR7 agonist with an EC50 of 238.1 nM. TLR7 agonist 27 shows weak agonistic activity against NOD2 (nucleotide-binding oligomerization domain 2) (EC50 of 6.2 μM). TLR7 agonist 27 is a potent immunostimulant, and can be used as a vaccine adjuvant and/or immunotherapeutic.
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ArMan
0 ImagesCat. No.: HY-175421ArMan is a co-activator of DC-SIGN (CD209) and TLR7. ArMan can selectively bind to DC-SIGN, promoting receptor-mediated endocytosis of the virus-like particle (VLP) platform, thereby enhancing co-binding with TLR7. ArMan can drive dendritic cell activation, shifting the immune response from humoral immunity to type 1 cellular immunity. ArMan can be used in melanoma research.
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Bazlitoran sodium
0 ImagesCat. No.: HY-177617ACAS No.: 1613607-40-1Synonyms: IMO-8400 sodiumBazlitoran sodium (IMO-8400 sodium) is an oligonucleotide-based TLR7/8/9 antagonist. Bazlitoran sodium blocks the activation of Toll-like receptors 7, 8, and 9. Bazlitoran sodium inhibits cytokine responses mediated by Toll-like receptors 7, 8, and 9. Bazlitoran sodium is associated with injection site reactions. Bazlitoran sodium improves moderate-to-severe plaque psoriasis.
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DS-7011a
0 ImagesCat. No.: HY-P992348DS-7011a is a selective inhibitor targeting TLR7. DS-7011a inhibits IL-6 production induced by TLR7 stimulation and related responses in B cells and plasmacytoid dendritic cells. DS-7011a is internalized in a TLR7-dependent manner and accumulates in B cells, various dendritic cell subsets, and monocytes/macrophages. DS-7011a can be used in research related to systemic lupus erythematosus (SLE).
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TLR7 agonist 5
0 ImagesCat. No.: HY-153070CAS No.: 2380231-67-2TLR7 agonist 5 (compound IIb-11) is an TLR7 agonist with an EC50 value of ~4 nM.
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TLR7 antagonist-1
0 ImagesCat. No.: HY-181796CAS No.: 3104353-70-7TLR7 antagonist-1 (Compound 44#) is an orally active, selective TLR7 antagonist with an IC50 value of 0.3 nM against TLR7. TLR7 antagonist-1 selectively binds to TLR7, inhibits its activation, and downregulates the c-Rel signaling pathway. TLR7 antagonist-1 downregulates the mRNA levels of proinflammatory cytokines IL-1β, IL-6, and TNF-α. TLR7 antagonist-1 alleviates Imiquimod (HY-B0180)-induced psoriasis-like skin lesions. TLR7 antagonist-1 is applicable to research related to psoriasis.
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TLR9-IN-2
0 ImagesCat. No.: HY-179209CAS No.: 2972638-16-5TLR9-IN-2 (Compound 20) is a selective inhibitor of Toll-like receptor 9 (TLR9) with IC50 values for TLR9, TLR7, and TLR8 of 25, 1400, and > 50,000 nM respectively. TLR9-IN-2 can be used for the study of fibrosis, autoimmune and inflammatory diseases.
