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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AXC-715 trihydrochloride
0 ImagesSynonyms: T785 trihydrochlorideAXC-715 (T785) trihydrochloride is a TLR7/TLR8 dual agonist. AXC-715 trihydrochloride 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.
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Gardiquimod diTFA
0 ImagesGardiquimod diTFA is an imidazoline TLR7/8 agonist. Gardiquimod diTFA inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 at concentrations below 10 μM.
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Bropirimine
0 ImagesSynonyms: U-54461; U-54461S; PNU-54461Bropirimine (U-54461; U-54461S; PNU-54461) is an orally active TLR7 agonist. Bropirimine inhibits RANKL-induced osteoclast differentiation of mouse bone marrow-derived macrophages (BMMs). Bropirimine exhibits dose-dependent direct inhibitory effects on colony formation of cultured KK-47 and 724 cells. Bropirimine can be used for the study of cancers and bone metabolic disorders such as osteoporosis.
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SM-324405
0 ImagesSM-324405 is a TLR7 agonistic antedrug (EC50 = 50 nM), with pEC50 values of 7.3 and 6.6 for human TLR7 and Rat TLR7, respectively. SM-324405 is used for immunoresearch of allergic diseases. An antedrug is defined as a locally active compound that is designed to be rapidly metabolized to an inactive form upon entry into the circulation and prevents systemic toxicity by losing its agonistic activity in a plasmatic environment.
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MTvkPABC-P5 TFA
0 ImagesCat. No.: HY-156693APurity: 98.78%MTvkPABC-P5d TFA, a TLR7 agonist, is an immune stimulant. MTvkPABC-P5d TFA can be used for synthesis of immune-stimulating antibody conjugates (ISACs).
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GSK2245035
0 ImagesGSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 is used for asthma.
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L07-2
0 ImagesL07-2 is a TLR7/8 agonist. L07-2 is a linker-toxin building block that can be used to synthesize immunostimulatory antibody conjugates (ISACs) for cancer research. L07-2 can be used to studies related to tumors such as non-small cell lung cancer.
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SMU-L11
0 ImagesSMU-L11 is a specific TLR7 agonist (EC50=0.024 μM), which recruits MyD88 adapter protein and activates downstream NF-κB and MAPK signaling pathways. In murine models, SMU-L11 significantly enhances immune cell activation and promotes the proliferation of CD4+ T and CD8+ T cells, thereby directly killing tumor cells and inhibiting tumor growth. SMU-L11 can be used for cancer research, and also has the potential for studying immune system diseases.
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TLR7 agonist 20 hydrochloride
0 ImagesCat. No.: HY-158694APurity: 99.86%TLR7 agonist 20 hydrochloride is a selective Toll-like receptor 7 (TLR7) agonist with an EC50 of 0.22 μM. TLR7 agonist 20 hydrochloride, as an immunostimulant and vaccine adjuvant, enhances the production of anti-spike protein antibodies, increases IgG2b and IgG2c levels, and thereby drives Th1-type immune responses in mice. TLR7 agonist 20 hydrochloride can be used in studies related to non-inflammatory potent vaccine adjuvants.
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MC-Val-Cit-PAB-Amide-TLR7 agonist 4 formic
0 ImagesCat. No.: HY-145960AMC-Val-Cit-PAB-Amide-TLR7 agonist 4 formic (example 15) is a HER2-TLR7 and HER2-TLR8 immune agonist conjugate.
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TLR7 agonist 4
0 ImagesTLR7 agonist 4 is a TLR7 agonist with pro-inflammatory cytokine-stimulating activity. TLR7 agonist 4 modulates TLR7 activity to stimulate the production of pro-inflammatory cytokines. TLR7 agonist 4 stimulates mouse bone marrow-derived macrophages to produce the pro-inflammatory cytokine TNFα. TLR7 agonist 4 can be conjugated with antibodies to form conjugates. TLR7 agonist 4 is applicable to cancer research.
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MC-Val-Cit-PAB-Amide-TLR7 agonist 4
0 ImagesCat. No.: HY-145960CAS No.: 2413016-49-4MC-Val-Cit-PAB-Amide-TLR7 agonist 4 (example 15) is a HER2-TLR7 and HER2-TLR8 immune agonist conjugate.
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TLR9 antagonist 1
0 ImagesCat. No.: HY-178037CAS No.: 3105410-45-2TLR9 antagonist 1 is a selective hTLR9 antagonist with an IC50 of 0.1 nM against hTLR9. TLR9 antagonist 1 exhibits favorable pharmacokinetic and pharmacodynamic properties. TLR9 antagonist 1 can be used in the research of systemic lupus erythematosus.
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Toll-like receptor modulator
0 ImagesToll-like receptor modulator is a modulator of TLR7/8, which modulates immune function.
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ODN 24888
0 ImagesCat. No.: HY-150744CAS No.: 1964506-30-6
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TLR7 agonist 6
0 ImagesCat. No.: HY-153071CAS No.: 2380231-86-5TLR7 agonist 6 (compound IIb-19) is an TLR7 agonist with an EC50 value of 1.0 nM.
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TLR7/8 agonist 8
0 ImagesTLR7/8 agonist 8 (compound 24m) is a potent toll-like receptor 7/8 (TLR7/8) dual agonist, with EC50s of 27 and 12 nM for hTLR7 and hTLR8, respectively. TLR7/8 agonist 8 can improve the antitumor activity of PD-1/PD-L1 blockade.
