Toll-like Receptor (TLR) Inhibitor

Saquinavir-d₉ (Ro 31-8959-d₉) is the deuterium labeled Saquinavir (HY-17007). Saquinavir (Ro 31-8959) is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir also has anti-inflammatory activity and can induce apoptosis of human red blood cells.

Tri(TLR4-IN-C34-C2-amide-PEG1)-amide-C3-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.

TLR7 agonist 32 (payload P3), a TLR7 agonist, is an ADC payload taht can be used in the synthesis of antibody-drug-conjugates (ADCs).

Cavrotolimod sodium is an immunostimulatory spherical nucleic acid (SNA) modified with type B CpG oligonucleotides designed to agonize TLR9 and elicit immune responses useful in oncology applications.

Astringin (trans-Astringin) (Standard) is the analytical standard of Astringin (HY-N4093). This product is intended for research and analytical applications. Astringin (trans-Astringin) is an orally active natural flavonoid compound. Astringin can inhibit the production of oxidative stress, inflammatory factors, etc. Astringin has multiple activities such as anti-oxidation, anti-inflammation, and anti-apoptosis. Astringin is also an inhibitor of ferroptosis. Astringin can be used in the research of diseases such as acute lung injury.

Tilsotolimod (IMO-2125) sodium is a TLR9 agonist. Tilsotolimod sodium activates the TLR9 signaling pathway, triggers downstream pro-inflammatory and immunostimulatory pathways, enhances the uptake and killing of cancer cells, and induces adaptive immune responses. Tilsotolimod sodium is applicable to research related to melanoma and colorectal cancer.

SARM1-IN-8 (compound 6) is a competitive SARM1 base-exchange inhibitor. SARM1-IN-8 shows competitive inhibition of SARM1^Δ1-27 activity with respect to the NAD⁺ substrate.

Aplysinol is an orally effective TLR4 signaling pathway inhibitor. Aplysinol reduces the expression of CD14, MyD88, and NF-κB p65, and downregulates the expression and secretion of TNF-α protein as well as the secretion of IL-1β. Aplysinol restores the phagocytic activity of Kupffer cells and reduces plasma endotoxin levels. Aplysinol alleviates alcohol-induced liver histopathological changes and inhibits the elevation of liver injury biomarkers, and can be used for research related to alcoholic liver disease.

JAK1-IN-16 (compound 4l) is an inhibitor of JAK1/STAT3 and effectively downregulates TLR4 protein expression..

DS-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).

NAB815 is a specific inhibitor of the Stx2a (K_d = 0.01 μM)/TLR4 interaction. NAB815 inhibits the neutrophil/Stx2a interaction (IC₅₀ = 0.057 μg/mL). NAB815 inhibits the formation of Stx2-containing extracellular vesicles (EVs) produced by leukocytes and platelets and reduces their toxic effects in cellular (Vero cells) and animal models (CD-1 mice). NAB815 reduces bacterial loads in the kidneys, urine, and bladders of Escherichia coli-infected mice. NAB815 is useful in the study of hemolytic uremic syndrome (HUS).

Saquinavir mesylate (Standard) (Ro 31-8959/003 (Standard)) is the analytical standard of Saquinavir mesylate (HY-17003). This product is intended for research and analytical applications. Saquinavir (Ro 31-8959) mesylate is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir mesylate also has anti-inflammatory activity and can induce apoptosis of human red blood cells.

TLR9-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.

Xanthine oxidase-IN-6 (Compound 6c) is a potent, orally active, mixed-type xanthine oxidase (XOD) inhibitor with an IC₅₀ value of 1.37 µM. Xanthine oxidase-IN-6 shows strong anti-hyperuricemia and renal protective activity.

ODN 21595 is a Guanine-Modified TLR7 and TLR9 inhibitor. ODN 21595 inhibits the release of IFN-α and IL-6 with no cytotoxic. ODN 21595 reduces the expression of CD86 and HLA-DR. ODN 21595 has the potential for the research of systemic lupus erythematosus (SLE).

Tilsotolimod sodium scrambled negative control is the sequence scrambled negative control of Tilsotolimod sodium.

Dendrocandin U is a bibenzyl compound found in Dendrobium officinale that exhibits anti-inflammatory activity and α-glucosidase inhibitory effect (IC₅₀ = 9.46 mM). Dendrocandin U inhibits the expression of TLR4 and MyD88 in the TLR4/MyD88/NF-kB pathway, suppresses the phosphorylation of NF-kB p65 and I-kBα, and blocks the nuclear translocation of NF-kB p65. Dendrocandin U inhibits M1 polarization, NO secretion, and TNF-α release in alveolar macrophages, and reduces inflammatory morphological changes in macrophages. Dendrocandin U promotes neurite outgrowth in PC12 cells. Dendrocandin U can be used for research on inflammation-related diseases and type 2 diabetes.

LM9 is a potent, orally active MyD88 inhibitor. LM9 blocks TLR4/MyD88 binding, MyD88 homodimer formation, and TLR4/MyD88/NF-κB signaling pathway activation. LM9 prevents atherosclerosis by regulating inflammatory responses and oxidative stress in macrophages. LM9 efficiently mitigates inflammatory responses and fibrosis in obesity-induced cardiomyopathy. LM9 can be used for fibrosis and atherosclerosis research.

PTPRO-IN-1 is a selective, orally active PTPRO inhibitor with an IC₅₀ of 0.16 μM. PTPRO-IN-1 exhibits IC₅₀ values of 2.4 μM, 2.33 μM and 2.13 μM against PTPN22, PTP1B and PTPRT, respectively, and shows almost no inhibitory activity against STEP/SSH2. PTPRO-IN-1 inhibits the TLR4/NF-κB signaling pathway in macrophages, ameliorates colonic pathological conditions and suppresses the secretion of pro-inflammatory cytokines by T cells. PTPRO-IN-1 can be used for the research of inflammatory bowel disease.

β-Funaltrexamine (β-FNA) is a blood-brain barrier-permeable, selective and irreversible μ-opioid receptor antagonist with immunomodulatory, anti-inflammatory and neuroprotective activities. β-Funaltrexamine inhibits p38 MAPK and TLR4 signaling by blocking μ-opioid receptors, and reduces the transcriptional activities of NF-κB, AP-1, CREB and Stat. Furthermore, β-Funaltrexamine inhibits iNOS activation and pro-inflammatory microglial polarization, converting microglia to an anti-inflammatory phenotype, thereby downregulating neuroinflammation and ameliorating neuronal degeneration. β-Funaltrexamine is widely applicable to research related to stroke, cerebral ischemia/reperfusion injury and neurodegenerative diseases.