TLR7 Inhibitor

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 .

Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro.

ABB071 is a humanized anti-CD180 monoclonal antibody. ABB071 can down-regulate the highly expressed TLR7 and IRF5 genes in systemic lupus erythematosus and induce the expression of PNPT1 and DNASE1L3 genes. ABB071 can inhibit the expression of genes related to the type I interferon pathway as well as interferon-stimulated genes (ISGs). ABB071 has anti-inflammatory activity and can reduce the levels of inflammatory cytokines. ABB071 can be used for research on systemic lupus erythematosus and psoriasis.

AT791 is a potent and orally bioavailable TLR7 and TLR9 inhibitor. AT791 inhibits TLR7 and 9 signaling in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro.

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.

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.

CL264 is a TLR7-specific agonist for innate immune signals research.

Hydroxychloroquine (sulfate) (Standard) is the analytical standard of Hydroxychloroquine (sulfate). This product is intended for research and analytical applications. Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro.

E104 (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.

ODN 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'.

ODN 24888 is an guanine-modified inhibitory oligonucleotides (INH-ODN), shows potent inhibition on TLR7/TLR9-mediated signaling. ODN 24888 impairs IFN-α level and NF-κB activation, inhibits IL-6 release. ODN 24888 involves in immune and inflammatory responses, can be used as a vaccine adjuvant.

TSI-13-57 is a pan-TLR inhibitor (IC₅₀: 2.7 μM, 6.03 μM, 7.37 μM, 6.38 μM for TLR9, TLR7, TLR2, TLR4, respectively). TSI-13-57 inhibits homodimerization of the TIR domains of MyD88. TSI-13-57 reduces systemic inflammatory responses in LPS-induced mice.

(S)-Hydroxychloroquine ((S)-HCQ) is the enantiomer of Hydroxychloroquine. Hydroxychloroquine, a synthetic antimalarial agent, inhibits Toll-like receptor 7/9 (TLR7/9) signaling, and shows efficiently inhibits SARS-CoV-2 infection in vitro.

(R)-Hydroxychloroquine is the enantiomer of Hydroxychloroquine. Hydroxychloroquine is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro.

ETI41 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC₅₀ = 0.63 μM) and TLR9 (IC₅₀ = 0.16 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI41 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI41 suppresses the expression of inflammation-associated genes and effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI41 can be used for autoimmune and inflammatory diseases research.

KBD4466 is an orally active potent TLR7 and TLR8 inhibitor with IC₅₀s of 0.9 nM and 2.8 nM, respectively. KBD4466 inhibits the expression of inflammatory cytokines IL-6 and IFN-α. KBD4466 improves disease progression and survival in the BXSB/MpJ mouse model of Systemic Lupus Erythematosus (SLE). KBD4466 can be used in the study of autoimmune diseases.

TLR7-IN-1 (Compound 16-A) is a TLR7 agonist with an EC₅₀ of 0.001 μM. TLR7-IN-1 is applicable to cancer-related research.

BI1543673 is an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor. BI1543673 can reduce the inflammatory response stimulated by TLR4 and TLR7/8 in human lung tissue. BI1543673 can decrease inflammatory signaling in a mouse model of lung inflammation induced by LPS.

TLR7 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.

ETI60 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.