TNF Receptor Inhibitor

Balinatunfib (SAR-441566) is an orally active inhibitor of TNFR1 signaling. By binding to the central pocket of the soluble TNFα (sTNFα) trimer, Balinatunfib stabilizes an asymmetric conformation, blocking its binding to TNFR1 (without affecting TNFR2) and thus inhibiting downstream pathways. Balinatunfib has anti-inflammatory activity, and can be used in the study of autoimmune diseases.

Belimumab (LymphoStat B) is a humanized IgG1λ monoclonal antibody against B-lymphocyte stimulator (BLyS) protein. Belimumab antagonizes BLyS activity in autoimmune diseases and B-lymphocyte malignancies. Belimumab can be used for systemic lupus erythematosus (SLE) research. The component ratio of this product is Active ingredient: Excipients = 1:1.0-1:1.2.

QNZ (EVP4593) shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC₅₀s of 11 and 7 nM, respectively. QNZ (EVP4593) is a neuroprotective inhibitor of SOC channel.

C25-140, a first-in-class, orally active, and fairly selective TRAF6-Ubc13 inhibitor, directly binds to TRAF6, and blocks the interaction of TRAF6 with Ubc13. C25-140 lowers TRAF6 activity, reduces NF-κB activation, and combats autoimmunity.

Rozanolixizumab (UCB7665), a humanized high-affinity anti-human neonatal Fc receptor (FcRn) monoclonal antibody (IgG4P), is used to the research of reducing pathogenic IgG in autoimmune and alloimmune diseases.

Desloratadine (Sch34117) is an orally active and selective H1 receptor antagonist (K_i=0.9 nM) with anti-inflammatory and anti-allergic activities. Desloratadine inhibits the release of histamine and LTC4 from human basophils and targets the regulatory signals of IL-4 and IL-13 production in basophils. Desloratadine significantly alleviates SAR symptoms in patients with concurrent asthma and can be used in the study of seasonal allergic rhinitis and chronic idiopathic urticaria.

Telitacicept (RC18) is a fully human TACI-Fc fusion protein. Telitacicept is a dual B lymphocyte stimulator (BLyS)/APRIL (a proliferation-inducing ligand) inhibitor that effectively blocks proliferation of B lymphocytes. Telitacicept can be used in research of B-cell autoimmune disease. The component ratio of this product is Active ingredient : Excipients = 1: 0.5-1: 0.8.

Frexalimab (SAR441344) is a second-generation monoclonal antibody targeting the CD40 ligand (CD40L) with a good safety profile. Frexalimab inhibits the binding between CD40 and CD40L to modulate immune response. Frexalimab is likely to help prevent the process of β-cell destruction. Frexalimab is proming for multiple sclerosis, lupus erythematosus, Sj gren’s syndrome and type I diabetes research.

UCB-9260, an orally active compound, inhibits TNF signaling by stabilising an asymmetric form of the trimer. UCB-9260 is selective for TNF over other superfamily members, and binds TNF with a similar K_d of 13 nM.

Utomilumab (PF 05082566) is a fully human IgG2 agonist monoclonal antibody that selectively binds to 4-1BB/CD137. Utomilumab can be used in the research of tumors such as follicular and other CD20⁺ non-Hodgkin lymphomas.

SPD304 is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC₅₀ of 22 μM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α.

Orientin is a neuroprotective agentinhibits which has anti-inflammation, anti-oxidative, anti-tumor, and cardio protection properties. Orientin inhibits the levels of IL-6, IL-1β and TNF-α. Orientin increases IL-10 level. Orientin exhibits neuroprotective effect by inhibits TLR4 and NF-kappa B signaling pathway. Orientin can used in study neuropathic pain.

Neochlorogenic acid is a natural polyphenolic compound found in dried fruits and other plants. Neochlorogenic acid inhibits the production of TNF-α and IL-1β. Neochlorogenic acid suppresses iNOS and COX-2 protein expression. Neochlorogenic acid also inhibits phosphorylated NF-κB p65 and p38 MAPK activation.

Golimumab (CNTO-148) is a potent human IgG1 TNFα antagonist monoclonal antibody. Golimumab has anti-inflammation activitity and inhibits IL-6 and IL-1β production. Golimumab acts via targeting and neutralizing TNF to prevent inflammation and destruction of cartilage and bone. Golimumab has the anticancer activity and induces cell apoptosis. Golimumab can be used for rheumatoid arthritis, Crohn's disease and cancer research.

Brentuximab (CAC-10) is a chimeric antibody targeting CD30. Brentuximab is conjugated with Monomethyl auristatin E (MMAE) (HY-15162) to form the antibody-drug conjugate Brentuximab vedotin (HY-P99107A). Brentuximab can be used for the research of cancer, such as lymphoma.

Astilbin is a flavonoid compound and enhances NRF2 activation. Astilbin also suppresses TNF-α expression and NF-κB activation.

Ianalumab (VAY-736) is a human, decarboxylated antibody against BAFF-R. Ianalumab can block the interaction between BAFF and BAFF-R and antagonize the apoptosis protection mediated by BAFF. Ianalumab exerts antibody-dependent cytotoxic (ADCC), depending on effector cell activation mediated by immune receptor tyrosine activation motif (ITAM).

Ozoralizumab (ATN-103) is an anti-TNFα humanized antibody. Ozoralizumab is a humanized trivalent nanobody compound that consists of two anti-human TNFα nanobodies and an anti-human serum albumin (HSA) nanobody. Ozoralizumab can be used in research of arthritis.

Infliximab (Anti-TNF-α) (Avakine (Anti-TNF-α)) is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α. Infliximab (Anti-TNF-α) prevents the interaction of TNF-α with TNF-α receptor (TNFR1 and TNFR2). Infliximab (Anti-TNF-α) has the potential for autoimmune, chronic inflammatory diseases and diabetic neuropathy research.

Povetacicept (ALPN-303) is an engineered Fc fusion protein containing the TACI domain, and acts as a dual APRIL/BAFF antagonist. The K_d value of Povetacicept for human BAFF is 59.3 pM, while its K_d value for human APRIL is 1.00 pM. Povetacicept reduces the activation, proliferation, differentiation and survival of B cells, and inhibits the production of immunoglobulins and autoantibodies. Povetacicept can be used in research related to autoimmune hemolytic anemia, immune thrombocytopenia, systemic lupus erythematosus, lupus nephritis and myasthenia gravis.