Sutimlimab, a first-in-class complement protein component 1, s subcomponent (C1s) inhibitor, can be used for the research of cold agglutinin disease. C1s is a serine protease which cleaves C4 and C2 to form the C3 convertase[1].
Mirococept (APT070) is an antibody targeting to complement system C3b/C4b, as well as a membrane-localizing C3 convertase inhibitor. Mirococept reduces the release of C-peptide and pro-inflammatory cytokines, and reduces the infiltration of inflammatory cells. Mirococept reduces intraislet inflammation, which is beneficial to islet transplantation. Mirococept also inhibits increased intestinal and pulmonary vascular permeability to reduce neutrophil influx[1][2].
Lampalizumab (RG 7417) is a humanised monoclonal antibody targeting complement Factor D in the alternative complement pathway. Lampalizumab binds an exosite and sterically blocks Factor B access to the active site. Lampalizumab can be used for age-related macular degeneration (AMD) research[1][2].
Vesencumab (MNRP-1685A) is IG1 antibody against neuropilin-1 (NRP-1). Vesencumab binds to NRP-1 and prevents the subsequent coupling of NRP-1 to VEGFR-2. Vesencumab has anti-angiogenic and anti-neoplastic activities. Vesencumab can be used in the research of metastatic solid tumors, including ovarian cancer[1][2].
Compstatin control peptide is a complement inhibitor.
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].
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].
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.
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].
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].
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].
C5aR-IN-2 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-2 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 49)[1].
Riliprubart (SAR445088) is an anti-C1s humanized monoclonal antibody that inhibits activated C1s in the proximal portion of the classical complement system. Riliprubart selectively inhibits activated C1s and prevents the enzymatic action of C1 on its substrates C4 and C2, thus inhibiting the formation of the classical pathway C3 convertase, C4b2a[1].
C5a Anaphylatoxin (human) is a pro-inflammatory peptide and a leukocyte chemoattractant. C5a Anaphylatoxin (human) can be used to study inflammation and immunity, such as allergic asthma[1][2].
Citrostadienol is a steroid compound with anti-inflammatory and anticomplementary activities. Citrostadienol demonstrates inhibition activities on classical complement pathway (IC50 of 46 nM)[1].
Avacopan (CCX168) is a potent, selective and orally available complement 5a receptor inhibitor with an IC50 of 0.1 nM.
CP-447697 is a lipophilic C5a receptor antagonist with an IC50 value of 31 nM. CP-447697 can be used for the research of inflammation[1].
Vemircopan is a complement factor D inhibitor[1].
C5aR-IN-3 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-3 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 89)[1].
Vilobelimab (CaCP-29, IFX-1) is a monoclonal anti-C5a antibody to the allergen C5a, a pro-inflammatory complement division product that plays a central role in mediating organ dysfunction. Vilobelimab acts as a C5a inhibitor, inhibiting neutrophil activation, chemotaxis, and reducing inflammatory signalling, and may be used in studies related to sepsis, COVID-19, etc[1].
BR103 is a potent, metabolically stable and highly selective small molecule agonist of complement C3a receptor (C3aR) with EC50 of 22 ± 8 nM; displays high selectivity for C3aR over C5aR; induces paw oedema and mast cell activation in vivo in rats.
Cemdisiran is an N-acetylgalactosamine (GalNAc) conjugated siRNA for the treatment of complement-mediated diseases by suppressing liver production of complement 5 (C5) protein.
Lipoteichoic acid, a cell wall component of Staphylococcus aureus, activates the complement system via C3 induction and CD55 inhibition[1].
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].
Novel potent and selective antagonist of human Complement C3a receptor