Zilucoplan (RA101495), a 15-amino acid macrocyclic peptide, is a potent complement component 5 (C5) inhibitor. Zilucoplan can be used in research of immune-mediated necrotising myopathy (IMNM)[1][2].
Olendalizumab (ALXN1007) is a mouse-derived and humanized IgG2-G4-κ antibody, targeting to Complement protein C5a (Ki=60 pM). Olendalizumab targets the complement inflammatory pathway. Moreover, Olendalizumab can be used for research of complement mediated disorder caused by corona virus[1][2].
Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary drug conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors[1][2][3].
JPE-1375 is a complement C5a receptor 1 (C5aR1) antagonist. JPE-1375 effectively inhibits polymorphonuclear leukocyte mobilization (EC50=6.9 µM) and reduces TNF levels (EC50=4.5 µM) in mice. JPE-1375 can be used in studies of autoimmune and inflammatory diseases[1].
AMY-101 TFA (Cp40 TFA), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation[1][2].
Eculizumab (Anti-Human C5, Humanized Antibody) is a long-acting humanized monoclonal antibody targeted against complement C5. Eculizumab inhibits the cleavage of C5 into C5a and C5b and hence inhibits deployment of the terminal complement system including the formation of membrane attack complex (MAC). Eculizumab has the potential for haemolysis research[1].
3-O-(2'E,4'Z-Decadienoyl)ingenol is a natural diterpene that exhibits significant anticomplement activity with an IC50 of 89.5 μM[1].
Factor B-IN-3 (Example 3 target compound) is a potent complement factor B inhibitor. Factor B-IN-3 can be used for the research of diseases related to inflammation and immunity[1].
FD-IN-1 (Compound 12) is a factor D (FD) inhibitor with an IC50 of 12 nM. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC50s of 7.7 and 6.5µM, respectively[1].
C3a (70-77) is an octapeptide corresponding to the COOH terminus of C3a, exhibits the specificity and 1 to 2% biologic activities of C3a.
Dexamethasone-d4 is deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
Factor B-IN-4 (Example 13 target compound) is a potent complement factor B inhibitor, with an IC50 of 1 μM. Factor B-IN-4 can be used for the research of diseases related to inflammation and immunity[1].
(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumorassociated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses[1].
Factor B-IN-2 (Example 1 target compound) is a potent complement factor B inhibitor, with an IC50 of 1.5 μM. Factor B-IN-2 can be used for the research of diseases related to inflammation and immunity[1].
Leukadherin-1 is a specific agonist of CR3 and the leukocyte surface integrin CD11b/CD18.
N-((Allyloxy)carbonyl)-N-methyl-L-alanine is a Alanine derivative. N-((Allyloxy)carbonyl)-N-methyl-L-alanine can be used for the synthesis of inhibitors of complement factor D. Complement factor D inhibitors can be used in the research of immune system related disease[1].
Tesidolumab (LFG316) is a fully-human IgG1/λ anti-C5 monoclonal antibody of 143 kDa (without glycosylation). Tesidolumab (LFG316) blocks cleavage of C5 and prevents subsequent formation of the membrane attack complex[1].
Pegcetacoplan is a pegylated complement C3 inhibitor peptide. Pegcetacoplan acts effect by binding with complement component 3 (C3) and its activation fragment C3b. Pegcetacoplan can be used for the research of complement-mediated diseases, including age-related macular degeneration, C3 glomerulopathy, Geographic atrophy (GA) and autoimmune haemolytic anaemia[1][2].
Novel potent and selective antagonist of human Complement C3a receptor
Factor B-IN-5 (Example 5 target compound) is a potent complement factor B inhibitor, with an IC50 of 1.2 μM. Factor B-IN-5 can be used for the research of diseases related to inflammation and immunity[1].
Avacincaptad pegol (ARC1905) is is an anti-C5 RNA aptamer that inhibits the cleavage of complement factor 5 (C5) into C5a and C5b. Avacincaptad pegol is being used for the study of age-related macular degeneration (AMD).
IONIS-FB-LRx is a specific antisense oligonucleotide (ASO) targeting complement factor B (CFB). IONIS-FB-LRx effectively reduces circulating levels of CFB. IONIS-FB-LRx can be used for geographic atrophy (GA) research[1][2].
AMY-101 (Cp40), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation[1][2].
C3a receptor agonist 1 (compound benzeneacetamide) is a potent C3a receptor agonist. C3a receptor agonist 1 has the potential for the research of acute inflammation[1].
Danicopan, a selective and orally active small-molecule factor D inhibitor, inhibits alternative pathway of complement (APC) activity. Danicopan has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS)[1].
Pozelimab (REGN3918) is a fully human IgG4 anti-C5 monoclonal antibody. Pozelimab binds to C5 and C5 variants with high affinity and blocks complement-mediated hemolysis. Pozelimab can be used for the research of complement-mediated diseases[1].
C5aR-IN-1 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-1 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 47)[1].
Factor D inhibitor 6 is a potent and selective, orally bioavailable inhibitor of Factor D with IC50 of 30 nM; is highly selective for human FD, showing no inhibition of factor B; efficiently block alternative pathway activation and prevent both C3 deposition onto, and lysis of, PNH erythrocytes; inhibits lipopolysaccharide-induced AP activation in FD-humanized mice.
Cyclosporin A-d3 is the d3-labeled Cyclosporin A (HY-B0579)[1].
C5a Receptor agonist, mouse, human is a biological active peptide. (This peptide is derived from the C-terminus of the chemokine, complement fragment 5 anaphylatoxin (C5a). This peptide functions as a C5a receptor agonist. C5a is a plasma protein involved in cellular inflammatory processes by inducing chemotaxis, degranulation of leukocytes, increased vascular permeability, and cytokine production. The cyclohexylalanine at position 5 is crucial to agonist function. Arg at the last position is of the d-isomer.)