Interleukin Related Antagonist

Raleukin (Kineret) is a recombinant, nonglycosylated human interleukin-1 receptor (IL-1R) antagonist. Raleukin significantly reduces neutrophil accumulation in blood vessels and brain infarct volume as well as improves motor coordination performance in ischemic stroke mice model. Anakinra can be used to study chronic inflammatory disorders like rheumatoid arthritis and cardiovascular recurrence post-myocardial infarction.

Tocilizumab (Anti-Human IL6R, Humanized Antibody) is an anti-human interleukin-6 receptor (IL-6R) neutralizing antibody, prevents binding of IL-6 to the IL-6R, thereby inhibiting both classic and trans-signaling. Tocilizumab (Anti-Human IL6R, Humanized Antibody) can be used for the treatment of rheumatoid arthritis. Tocilizumab is remarkablely effective for the study of severe COVID-19 (coronavirus disease).

Icotrokinra (JNJ-77242113) is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC₅₀=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC₅₀ of 18.4 pM. Icotrokinra exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease.

Bimekizumab (Anti-Human IL17A/IL-17F Recombinant Antibody) is a humanised monoclonal antibody, can selectively neutralises IL-17A and IL-17F. Both of them are pro-osteogenic with respect to human periosteum-derived cell (hPDC) differentiation. Thus Bimekizumab blocks the inflammation-driven osteogenic differentiation.

Lusvertikimab (OSE-127) is a humanized IL7R monoclonal antibody. Lusvertikimab is not internalized by target cells and prevents IL7R heterodimerization and subsequent downstream signaling. Lusvertikimab has anti-leukemic efficacy and has the potential for B cell precursor acute lymphoblastic leukemia (BCP-ALL) research.

IL-17A antagonist 1 is an interleukin-17A (IL-17A) antagonist with an IC₅₀ of 1.14 μM and a K_d of 0.66 μM. IL-17A antagonist 1 binds specifically and exclusively to the IL-17A homodimer at its central dimer interface pocket, induces a large conformational change that widens the pocket, and disrupts the IL-17A/IL-17RA interaction. IL-17A antagonist 1 does not bind to IL-17F or IL-17RA.

Bempikibart (ADX-914) is a fully human anti-IL-7Rα antibody that re-regulates adaptive immune function by blocking signaling mediated by both IL-7 and thymic stromal lymphopoietin (TSLP). Bempikibart can be used for the study of atopic dermatitis and alopecia areata.

S7 is an inhibitory polypeptide targeting IL-6R, which specifically binds to IL-6R and its A chain (gp80/IL-6RA) to block its signal transduction. S7 inhibits IL-6-mediated anti-apoptosis (apoptosis), angiogenesis and the expression of VEGF-A, blocks related survival signaling pathways, and enhances the sensitivity of cancer cells to chemotherapeutic drugs. S7 can be applied to the research of related diseases such as cervical cancer, multiple myeloma, Kaposi's sarcoma, prostate cancer and basal cell carcinoma.

Tildrakizumab (SCH 900222) is a humanized anti-IL-23 (p19 subunit) monoclonal antibody. IL-23 is a critical cytokine to maintain the Th17 cell phenotype. Tildrakizumab has high-affinity for single-chain IL-23 (K_d: 136 pM). Tildrakizumab is effective against moderate to severe plaque psoriasis.

Secukinumab (Anti-Human IL-17A) is a fully human anti-interleukin-17A monoclonal antibody. Anti-Human IL-17A can be used for research in psoriasis pathogenesis.

Reslizumab (Sch 55700) is humanized monoclonal antibodies that target interleukin-5 (IL-5) for the treatment of eosinophilic asthma. Reslizumab is effective in neutralizing the function of IL-5. Reslizumab has high binding affinity for human IL-5, with K_D values of 109 pM and 4.3 pM in the the Biacore surface plasmon resonance and Kinetic Exclusion Assay, respectively.

Simepdekinra (LY4100511; DC-853) is an IL-17A antagonist. Simepdekinra can be used in the research of moderate to severe plaque-type psoriasis.

Erepdekinra is an interleukin-17A (IL-17A) receptor antagonist.

Anti-Mouse IL-4Rα Antibody (REGN1103) is a mouse homologous antibody targeting IL-4Rα, as well as an inhibitor of IL-4 signaling. Anti-Mouse IL-4Rα Antibody (REGN1103) can be used in studies related to alveolar rhabdomyosarcoma.

Elubrixin tosylate (SB-656933 tosylate) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin tosylate inhibits neutrophil CD11b upregulation (IC₅₀ of 260.7 nM) and shape change (IC₅₀ of 310.5 nM). Elubrixin tosylate has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation.

Goflikicept (RPH 104) is a fusion protein that selectively binds and inactivates both circulating IL-1β and IL-1α. Goflikicept has the potential for the research of ST-segment elevation myocardial infarction (STEMI).

IL-17A antagonist 3 is an IL-17A antagonist, compound 3.

4L2-P13D is an IL-11 antagonist with an IC₅₀ of 2.8 μM. 4L2-P13D has a K_D of 11 nM for hIL-11. 4L2-P13D exhibits antifibrotic and renoprotective activities. 4L2-P13D can be used in the research of renal fibrosis.

36R-D481 is a competitive and orthosteric antagonist of IL-36R, effectively inhibiting IL-36 signaling. 36R-D481 can inhibit IL-36α and IL-36γ but not IL-36β induced IL-8 release.

EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 with an IC₅₀ value of 1.1 nM. EP4 receptor antagonist 7 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC₅₀ value of 0.9 nM. EP4 receptor antagonist 7 decreases PGE2-induced expression of mRNA encoding IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C) motif ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase-1 (Arg1), in RAW 264.7 macrophages. EP4 receptor antagonist 7 combined with an anti-PD-1 antibody inhibits tumor growth and increases infiltration of CD⁸⁺ T cells into tumors in a CT26 murine colon cancer model.