Toll-like Receptor (TLR) Inhibitor

CU-CPT22 (Standard) is the analytical standard of CU-CPT22 (HY-108471). This product is intended for research and analytical applications. CU-CPT22 is a potent protein complex of toll-like receptor 1 and 2 (TLR1/2) inhibitor, and competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with a K_i of 0.41 µM. CU-CPT22 blocks Pam3CSK4-induced TLR1/2 activation with an IC₅₀ of 0.58 µM.

Famotidine-¹³C (MK-208-¹³C) is the ¹³C-labeled Famotidine (HY-B0377). Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer.

M62812 (Standard) is the analytical standard of M62812 (HY-103639A). This product is intended for research and analytical applications. M62812 is a toll-like receptor 4 (TLR4) signaling inhibitor. M62812 inhibits endothelial and leukocyte activation and prevents lethal septic shock in mice. M62812 can reduces LPS-induced coagulation and inflammatory responses. M62812 can be used for the research of sepsis.

PROTAC HDAC6 degrader-13 is a selective CRBN-recruiting HDAC6 PROTAC degrader. PROTAC HDAC6 degrader-13 does not affect class I HDACs. PROTAC HDAC6 degrader-13 inhibits TLR-NLRP3 inflammatory signaling. PROTAC HDAC6 degrader-13 is useful for research on acute myeloid leukemia.

Chloroquine (dihydrochloride) (Standard) is the analytical standard of Chloroquine (dihydrochloride). This product is intended for research and analytical applications. Chloroquine dihydrochloride is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine dihydrochloride is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine dihydrochloride is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].

Saquinavir-¹³C₆ (Ro 31-8959-¹³C₆) is ¹³C 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.

Nalmefene (Standard) is the analytical standard of Nalmefene. This product is intended for research and analytical applications. Nalmefene is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene is used for opioid overdose and alcohol dependence.

HMGB1-IN-3 (compound E) is a glycyrrhizic acid derivative with strong inhibitory activity against HMGB1 (high mobility group protein 1) and can be used in the study of intracerebral hemorrhage.

Desethyl chloroquine (Standard) is the analytical standard of Desethyl chloroquine. This product is intended for research and analytical applications. Desethyl chloroquine is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine possesses antiplasmodic activity.

Isofraxidin (Standard) is the analytical standard of Isofraxidin. This product is intended for research and analytical applications. Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells. Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation.

Chitohexaose hexahydrochloride is a small molecular polysaccharide. Chitohexaose hexahydrochloride inhibits the binding of AgW to TLR4. Chitohexaose hexahydrochloride upregulates IL-10, inhibits LPS-induced upregulation of ROS, induces alternative activation of macrophages/monocytes, and suppresses LPS-induced production of TNF-α, IL-1β and IL-6. Chitohexaose hexahydrochloride reverses the mortality of mice challenged with APAP or LPS. Chitohexaose hexahydrochloride can be used in research related to Acetaminophen (HY-66005)-induced hepatotoxicity and endotoxemia.

Trimebutine (Standard) is the analytical standard of Trimebutine (HY-B0380). This product is intended for research and analytical applications. Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca²⁺ channels and large-conductance calcium-activated potassium channels (BK_Ca channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

Desethyl chloroquine (diphosphate) (Standard) is the analytical standard of Desethyl chloroquine (diphosphate). This product is intended for research and analytical applications. Desethyl chloroquine diphosphate is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine diphosphate possesses antiplasmodic activity.

Wilforlide A (Standard) is the analytical standard of Wilforlide A. This product is intended for research and analytical applications. Wilforlide A is a bioactive triterpene isolated from Tripterygium wilfordii Hook f. Wilforlide A has anti-inflammatory and immune suppressive effects.

C29 (Standard) is the analytical standard of C29 (HY-100461). This product is intended for research and analytical applications. C29 is a Toll-like receptor 2 (TLR2) inhibitor. C29 blocks hTLR2/1 and hTLR2/6 signaling with IC50s of 19.7 and 37.6 μM, respectively.

Pamidronic acid (Standard) is the analytical standard of Pamidronic acid. This product is intended for research and analytical applications. Pamidronic acid, the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronic acid significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of OPG in cartilage and subchondral bone, and inhibiting the expression of RANKL and MMP-9 in both tissues, as well as TLR-4 in cartilage, thereby alleviating cartilage degeneration. Additionally, Pamidronic acid can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma.

MD2-IN-1 (Standard) is the analytical standard of MD2-IN-1 (HY-103483). This product is intended for research and analytical applications. MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a K_d of 189 μM for the recombinant human MD2 (rhMD2).

Enpatoran (Standard) is the analytical standard of Enpatoran (HY-134581). This product is intended for research and analytical applications. 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 pharmacoK_inetic properties in vivo. Enpatoran can be used for both innate and adaptive autoimmunity blocK_ing research .

Atazanavir-d₂₄ (BMS-232632-d₂₄) is deuterium labeled Atazanavir. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.