TLR8

TLR8 is an endosomal pattern-recognition receptor that detects RNA degradation products and activates innate immune signaling in human myeloid cells^[1]^[2]. Mechanistically, RNase T2 processes single-stranded RNA into uridine and purine-2′,3′-cyclophosphate-terminated oligoribonucleotides, which engage two TLR8 ligand-binding pockets^[1]^[2]. In monocytes, TLR8 and TLR7 activate distinct pathways during RNA virus infection, making isoform-specific analysis essential for antiviral and inflammatory research^[3]. Disease studies show that TLR8 gain-of-function variants cause neutropenia, antibody deficiency, lymphoproliferation, and bone marrow failure, linking excessive TLR8 signaling to human immunopathology^[4]. For experimental applications, selective synthetic agonists help distinguish TLR8 biology from TLR7 biology by separating target-cell selectivity and cytokine-induction profiles^[5].- TLR8 links RNA degradation sensing to innate immune activation in human myeloid cells.- Isoform-specific assays distinguish TLR8 signaling from related TLR7 pathways.- Agonist tools support controlled studies of cytokine induction and immune-cell activation.

References:

[1]. Greulich W, et al. TLR8 Is a Sensor of RNase T2 Degradation Products. Cell. 2019 Nov 27;179(6):1264-1275.e13. [Content Brief]

[2]. Tanji H, et al. Toll-like receptor 8 senses degradation products of single-stranded RNA. Nat Struct Mol Biol. 2015 Feb;22(2):109-15. [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]. Aluri J, et al. Immunodeficiency and bone marrow failure with mosaic and germline TLR8 gain of function. Blood. 2021 May 6;137(18):2450-2462. [Content Brief]

[5]. Gorden KB, et al. Synthetic TLR agonists reveal functional differences between human TLR7 and TLR8. J Immunol. 2005 Feb 1;174(3):1259-68. [Content Brief]

TLR8 Related Products (65):

By Type:	Pan (25) Selective (13)
By Effects:	Inhibitors (8) Agonists (41) Antagonists (8) Activators (4) Modulator (1) Ligand (1)

Cat. No.	Product Name	Effect	Purity

HY-13740

Resiquimod	Agonist	99.95%
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.

HY-134581

Enpatoran	Inhibitor	99.80%
Enpatoran (M5049) is a potent, orally active and dual TLR7/8 inhibitor with IC₅₀s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran exhibits excellent pharmacokinetic properties in vivo. Enpatoran can be used for both innate and adaptive autoimmunity blocking research .

HY-13773

Motolimod	Agonist	98.10%
Motolimod (VTX-2337;VTX-378) is a selective Toll-like receptor 8 (TLR8) agonist, with an EC₅₀ of approximately 100 nM.

HY-109104

Telratolimod	Agonist	98.85%
Telratolimod (MEDI9197) is a potent toll like receptors 7/8 (TLR7/8) agonist, with antitumor activity.

HY-109137

Selgantolimod	Agonist	98.18%
Selgantolimod (GS-9688) is an orally active, potent and selective toll-like receptor 8 (TLR8) agonist for the treatment of hepatitis B virus (HBV) and human immunodeficiency virus (HIV) infection.

HY-145960A

MC-Val-Cit-PAB-Amide-TLR7 agonist 4 formic	Agonist
MC-Val-Cit-PAB-Amide-TLR7 agonist 4 formic (example 15) is a HER2-TLR7 and HER2-TLR8 immune agonist conjugate.

HY-P992458

SBT8230	Agonist
SBT8230 is an ASGR1-targeted TLR8 agonist and an ASGR1-TLR8 immune TAC conjugate. SBT8230 achieves liver enrichment via conjugation with an anti-ASGR1 antibody, activates myeloid cells and induces anti-HBV immune responses. SBT8230 is applicable to research on chronic hepatitis B infection. The corresponding isotype control is: Human lgG1 kappa,lsotype Control (HY-P99001).

HY-183276

TLR8 antagonist-2	Antagonist
TLR8 antagonist-2 (Compound 35) is a selective TLR8 antagonist with an IC₅₀ of 0.032 μM against hTLR8. TLR8 antagonist-2 potently inhibits TLR8-dependent NF-κB activity in cells stimulated with TL8-506 (HY-20457). TLR8 antagonist-2 can be used in research related to inflammatory and immune diseases.

HY-134581A

Enpatoran hydrochloride	Inhibitor	99.42%
Enpatoran (M5049) hydrochloride is a potent, orally active and dual TLR7/8 inhibitor with IC₅₀s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran hydrochloride is inactive against TLR3, TLR4 and TLR9. Enpatoran hydrochloride can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran hydrochloride exhibits excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be used for both innate and adaptive autoimmunity blocking research.

HY-128799

CL097	Agonist	99.90%
CL097, 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.

HY-160229

ssRNA40 sodium	Activator	98.34%
ssRNA40 sodium (R-1075 sodium) is a single-stranded RNA40 derived from HIV-1. ssRNA40 sodium activates the TLR7, TLR8, TLR2, RIG-I, MDA5, MyD88, Caspase-3, IRE1α, NLRP3 inflammasome and IRF7 signaling pathways. ssRNA40 sodium alters mRNA expression in neutrophils, induces pro-inflammatory cytokines, ROS, autophagy (autophagy), pyroptosis (pyroptosis), neuronal death, neurodegeneration, aggregate formation and NK cell activation. ssRNA40 sodium activates the expression of CD62L, CD11b, CD69, MX1, OAS1, ATG7, LC3B and XBP1 in immune cell and neuronal populations. ssRNA40 sodium causes cortical neuron loss and axonal damage in mice in a TLR7-dependent manner. ssRNA40 sodium can be used in research on HIV-1 infection, neurodegeneration, COVID-19 and HIV-associated neurological disorders.

HY-103697

Gardiquimod		99.91%
Gardiquimod is an imidazoline TLR7/8 agonist. Gardiquimod inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 at concentrations below 10 μM.

HY-20457

TL8-506	Agonist
TL8-506 is a specific TLR8 agonist with an EC₅₀ of 30?nM. TL8-506 has immunomodulatory effects and can be used in the study of tuberculosis and cancer immunotherapy.

HY-103698

TLR7/8 agonist 1	Agonist	98.42%
TLR7/8 agonist 1 is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.

HY-112667

CU-CPT-9a	Antagonist	99.74%
CU-CPT-9a is a specific TLR8 antagonist, with an IC₅₀ of 0.5 nM.

HY-139323

TLR7/8-IN-1	Inhibitor	99.92%
TLR7/8-IN-1 is a crystalline from of a TLR7/TLR8 inhibitor extracted from patent WO2019220390, compound 2b. TLR7/8-IN-1 can be used for the research of autoimmune disease.

HY-117066

CL075	Agonist	99.18%
CL075 (3M002) is a selective TLR8 agonist with immunomodulating properties. CL075 triggers a MyD88-dependent signaling pathway to elicit production of inflammatory cytokines and type I interferons (IFNs) via activation of NF-κB and IRF7, respectively.

HY-103698A

TLR7/8 agonist 1 dihydrochloride	Agonist	99.70%
TLR7/8 agonist 1 dihydrochloride is a toll-like receptor TLR7/TLR8 dual-agonistic imidazoquinoline.

HY-13740G

Resiquimod (GMP)	Agonist
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.

HY-112050

CU-CPT-8m	Antagonist	99.98%
CU-CPT-8m is a specific TLR8 antagonist, with an IC₅₀ of 67 nM.

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