TNF Receptor Antagonist

R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.

TAPI-1 is a broad-spectrum MMP inhibitor and NF-κB p65 inhibitor that targets ADAM17/TACE, ADAM10 and other proteins. TAPI-1 reduces the proteolytic cleavage of membrane-bound TNF-α, decreases TNF-α levels, inhibits NF-κB pathway activation, and downregulates profibrotic markers. TAPI-1 reduces the proportion of proinflammatory immune cells, alleviates cardiac and airway fibrosis, and improves cardiac function after myocardial infarction. Meanwhile, TAPI-1 inhibits the viability, migration and invasion of esophageal squamous cell carcinoma cells, enhances the chemosensitivity of Cisplatin (HY-17394), induces apoptosis, and shows low toxicity to normal esophageal epithelial cells. TAPI-1 can be widely used in studies related to myocardial infarction-induced heart failure, severe traumatic tracheal stenosis, esophageal squamous cell carcinoma and other conditions.

Atrosab is a humanized IgG1 antagonistic anti-TNFR1 antibody. Atrosab inhibits TNF-mediated Apoptosis induction and IL-6 and IL-8 production. Atrosab reduces neurological deficits. Atrosab can be used for research of inflammatory disease. The recommend isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).

L-Threonic acid magnesium (Magnesium L-threonate) is the enantiomer of Threonic acid and the metabolite of vitamin C (HY-B0166). L-Threonic acid magnesium is a magnesium supplementation, that improves the brain magnesium concentration, inhibits the activation of TNF-α/NF-κB signaling pathway. L-Threonic acid magnesium can be used in research of Alzheimer’s disease. L-Threonic acid magnesium is orally active.

Lubiprostone (SPI-0211) increases intestinal fluid secretion through generation of CIC-2/CFTR and activation of cAMP signaling pathway. Lubiprostone inhibits myeloperoxidase (MPO) activity, downregulates Indomethacin (HY-14397)-induced iNOS and TNFα expression. Lubiprostone can be used for chronic constipation research.

L-Norvaline is the inhibitor for arginase, that promotes the production of NO, reduces oxidative stress, improves insulin resistance, and exhibits antioxidant and anti-hyperglycemic effects. L-Norvaline can be used in research of Alzheimer’s disease.

Tanimilast (CHF-6001) is an orally active and selective phosphodiesterase 4 inhibitor (IC₅₀=0.026 nM) with robust anti-inflammatory activity and suitable for topical pulmonary administration. Tanimilast increases cellular cAMP levels, and inhibits NF-κB signaling pathway. Tanimilast is used for the research of obstructive lung diseases.

WP9QY, TNF-a Antagonist, TNF-a Antagonist is a biological active peptide. (This cyclic peptide is designed to mimic the most critical tumor necrosis factor (TNF) recognition loop on TNF receptor I. It prevents interactions of TNF with its receptor. This TNF antagonist is a useful template for the development of small molecular inhibitors to prevent both inflammatory bone destruction and systemic bone loss in rheumatoid arthritis.)

WP9QY is an inhibitor targeting TNFα and RANKL, which blocks the TNFα-TNFR1 interaction and inhibits TNFα-mediated apoptosis, cytotoxicity and bone destruction. WP9QY inhibits osteoclastogenesis and promotes osteoblast differentiation, induces chondrocyte proliferation and glycosaminoglycan production, and synergizes with TGF-β3 to promote chondrogenesis. WP9QY effectively repairs full-thickness articular cartilage defects in rabbits via intra-articular injection, and inhibits methylmercury-induced reduction of NeuN-positive cells in mouse brain slices. WP9QY can be applied to the research of diseases related to methylmercury-induced neuronal death, cartilage injury, osteoarthritis and bone loss.

GSK1995057 is a human monoclonal antibody (mAb) targeting TNFRSF1A. GSK1995057 selectively binds to TNFR1, blocks the binding of TNF-α and LT-α, and does not interfere with TNFR2 signaling. GSK1995057 inhibits the activation of NF-κB, JNK and MAPK pathways, alleviates apoptosis (apoptosis) and inflammatory responses (inhibiting IL-1β, IL-6, IL-10, TNF-α), and prevents viability loss of human nucleus pulposus cells. GSK1995057 inhibits the expression of cytokines and neutrophil adhesion molecules in human pulmonary microvascular endothelial cell monolayers, and reduces inflammatory responses and lung injury symptoms in non-human primates. GSK1995057 forms complexes with HAVH autoantibodies, thereby activating TNFR1 and triggering the release of cytokines and IL-8 in human cells. GSK1995057 can be used in research related to intervertebral disc degeneration and acute lung injury.

L-Norvaline-d₅ is the deuterium labeled L-Norvaline. L-Norvaline is the inhibitor for arginase, that promotes the production of NO, reduces oxidative stress, improves insulin resistance, and exhibits antioxidant and anti-hyperglycemic effects. L-Norvaline can be used in research of Alzheimer’s disease.

GSK2862277 is a human monoclonal antibody (mAb) targeting TNFRSF1A. GSK2862277 increases neutrophil extracellular trap formation and alveolar macrophage phagocytosis. GSK2862277 can be used in Acute lung injury and Acute Respiratory Distress Syndrome (ARDS) research. Recommended isotype control: VHH-hFc.

PF-07329640 is a humanized monoclonal antibody inhibitor targeting TNFRSF3. PF-07329640 can be used for advanced/metastatic solid tumors like non-small cell lung cancer (NSCLC) and colorectal cancer (CRC) research.

sEH inhibitor-19 (Compound (R)-14i) is an orally active inhibitor for soluble epoxide hydrolase (sEH) with an IC₅₀ of 1.2 nM. sEH inhibitor-19 inhibits the expression of TNF-α and IL-6, exhibits anti-inflammatory activity in mouse acute pancreatitis or Carrageenan (HY-125474)-induced edema models.

EGFR-IN-144 (Compound 4B) exhibits inhibitory activities against EGFR (IC₅₀=0.639 µg/mL) and tubulin polymerization (IC₅₀=7.339 µg/mL). EGFR-IN-144 exhibits cytotoxicity in multiple cancer cell with GI₅₀ of nanomolare levels. EGFR-IN-144 downregulates the expressions of mTOR, TNF-α, and IL-6, arrests the cell cycle at G1/S phase, and induces apoptosis.

Epaldeudomide (Compound A406) is the inhibitor for TNF-α (>50% inhibition rate at 100 nM). Epaldeudomide inhibits the proliferation of cancer cells MM.1S (IC₅₀ < 300 nM), WSU-DLCL-2 (IC₅₀ < 100 nM) and Rec-1 (IC₅₀ < 100 nM). Epaldeudomide exhibits antineoplastic activity.

DT-5461 is an IL-1 and TNF-α antagonist. DT-5461 competitively binds lipid A-binding sites on macrophage receptors, blocks LPS (HY-D1056)-initiated signaling, inhibits LPS-induced cytokine release, prevents LPS-induced serum cytokine production in mice, and protects against LPS-induced lethal endotoxemia. DT-5461 can be used for the research of lethal endotoxemia, medullary tubular mammary carcinoma, poorly differentiated colon adenocarcinoma, squamous-cell lung carcinoma, and gelatinous gastric adenocarcinoma.

L-Norvaline (Standard) is the analytical standard of L-Norvaline (HY-Y0399). This product is intended for research and analytical applications. L-Norvaline is the inhibitor for arginase, that promotes the production of NO, reduces oxidative stress, improves insulin resistance, and exhibits antioxidant and anti-hyperglycemic effects. L-Norvaline can be used in research of Alzheimer’s disease.

PIYLGGVFQ is a peptide inhibitor for TNF-α. PIYLGGVFQ inhibits TNF-α-mediated apoptosis, NF-κB nuclear translocation and activation. PIYLGGVFQ exhibits anti-arthritic activity in the CIA mouse model.

Paeoniflorin-6′-O-benzene sulfonate (CP-25) is the inhibitor for G protein-coupled receptor kinase 2 (GRK2) that inhibits the translocation of GRK2 to the cell membrane, inhibits JAK1/STAT3 signaling pathway. Paeoniflorin-6′-O-benzene sulfonate inhibits IL-17A/CXCL2-induced proliferation of HaCaT. Paeoniflorin-6′-O-benzene sulfonate reduces the levels of inflammatory factors and chemokines such as IL-17A, IL-17F, IFN-γ, TNF-α, IL-22, IL-23, CXCL2, CXCL3 and CXCL9, alleviates Imiquimod (HY-B0180)-induced psoriasis in mouse model.