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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Resiquimod (GMP)
0 ImagesCat. No.: HY-13740GCAS No.: 144875-48-9Synonyms: R848 (GMP); S28463 (GMP)Resiquimod (R848) (GMP) is Resiquimod (HY-13740) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist. Resiquimod (GMP) can induce human mMDSC to mature into inflammatory macrophages.
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DSR-6434
0 ImagesDSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect.
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Loxoribine
0 ImagesSynonyms: 7-Allyl-8-oxoguanosine; RWJ 21757Loxoribine (7-Allyl-8-oxoguanosine) is a guanosine analog with anti-viral and anti-tumor activities. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist.
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CL097 hydrochloride
0 ImagesCL097, a potent TLR7 and TLR8 agonist, induces pro-inflammatory cytokines in macrophages. CL097 induces NADPH oxidase priming, resulting in an increase of the fMLF-stimulated ROS production.
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BBIQ
0 ImagesBBIQ is a imidazoquinoline compound and a potent and selectively toll-like receptor 7 (TLR7) agonist with an EC50 of 59.1 nM for human TLR7. BBIQ is a powerful vaccine adjuvant that enhances innate immune responses.
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ORN 06 sodium
0 ImagesCat. No.: HY-160227AORN 06 (sodium) s a synthetic single-stranded U-rich RNA and contains 6 repeats of the UUGU sequence motif. The GU-rich oligoribonucleotides (ORNs) are able to stimulate TLR7.
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TLR7 agonist 1
0 ImagesTLR7 agonist 1 is a selective TLR7 agonist with an LEC value of 90 nM. TLR7 agonist 1 activates downstream immune regulation and shows no activity against TLR8. TLR7 agonist 1 induces endogenous IFN-α production in mice.
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1V209
0 ImagesSynonyms: TLR7 agonist T71V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects. 1V209 can be conjugated with various polysaccharides to improve its water solubility, and enhance its efficacy, and maintain low toxicity.
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AZD8848
0 ImagesAZD8848 is a selective toll-like receptor 7 (TLR7) anteagent agonist which is developed for the research of asthma and allergic rhinitis.
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E104
0 ImagesE104 (compound 1) is a potent and selective TLR7 agonist. E104 can be delivered by antibody-drug conjugate (ADC) technology to elicit potent anticancer activity. E104 induces the activation of mouse macrophages and hPBMCs.
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TLR7 agonist 3
0 ImagesTLR7 agonist 3 (compound 2) is a TLR7 agonist and can be used for the stuy of cancers.
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Resiquimod-d5
0 ImagesSynonyms: R848-d5; S28463-d5Resiquimod-d5 is deuterium labeled Resiquimod. 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.
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ODN 20844
0 ImagesCat. No.: HY-150736CAS No.: 1964506-29-3ODN 20844, a guanine-modified inhibitory oligonucleotide (INH-ODN), is a TLR7 and TLR9 (Toll-like receptor) inhibitor, and its parent is INH-ODN 2088. ODN 20844 disrupts TLR7- and TLR9-mediated immune cell immune responses. ODN 20844 sequence: 5'-TCCTGGCGc7GGGAAGT-3'.
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TLR7/8 agonist 4
0 ImagesTLR7/8 agonist 4 (compound 41) is a potent TLR7/8 agonist. TLR7/8 agonist 4 has anti-cancer activity.
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CU-115
0 ImagesCU-115 is a potent TLR8 antagonist (IC50=1.04 µM), and shows selective for TLR8 over TLR7 (IC50=>50 µM). CU-115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells.
