Complement System

TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM).

Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity.

JR14a is a potent thiophene antagonist of human complement C3a receptor.

Iptacopan (LNP023) hydrochloride is a highly selective small-molecule inhibitor of factor B (FB) with an IC₅₀ of 10nM and a KD of 7.9nM.

Complement factor D-IN-2 is an inhibitor of complement factor D extracted from patent WO2015130838A1, compound 190.

POT-4 (AL-78898A), a Compstatin derivative, is a potent inhibitor of complement factor C3 activation.

Vemircopan (ALXN2050) is an orally active complement factor D inhibitor.

Eculizumab (Anti-Human C5, Humanized Antibody) is a long-acting humanized monoclonal antibody targeted against complement C5.

Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM.

Factor B-IN-1 is a Factor B inhibitor extracted from patent WO2013164802A1, Example 24.

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.

Cemdisiran is an N-acetylgalactosamine (GalNAc) conjugated siRNA for the treatment of complement-mediated diseases by suppressing liver production of complement 5 (C5) protein.

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.

ARC 186 is a nucleic acid adapter that serves as an efficient complement inhibitor by blocking the activation of C5 catalyzed by convertase.

NRP1 antagonist 1 (compound 12a) is an effective NRP1 inhibitor with an IC50 of 19.1 μM. It has potential for use in cancer research.

Pelecopan (BCX9930) is an effective and selective complement factor D inhibitor with oral activity. Its IC50 value is 14.3 nM. Pelecopan can target complement factor D to prevent intravascular and extravascular hemolysis in PNH, as well as other diseases mediated by alternative pathways.

Ravulizumab (ALXN1210) is a humanized monoclonal antibody that binds specifically and with high affinity to human complement protein C5. Ravulizumab can be used in the research of paroxysmal nocturnal hemoglobinuria, atypical hemolytic uremic syndrome, and myasthenia gravis.

Tesidolumab (LFG316) is a fully human IgG1/Λ monoclonal antibody against C5, with a molecular weight of 143 kDa (excluding glycosylation). Tesidolumab (LFG316) blocks the cleavage of C5, preventing the subsequent formation of membrane attack complex.

Vesencumab (MNRP-1685A) is an IG1 antibody targeting neuropilin-1 (NRP-1). Vesencumab binds to NRP-1 and blocks its coupling with VEGFR-2. Vesencumab has antiangiogenic and antitumor activity. Vesencumab can be used for research on metastatic solid tumors, including ovarian cancer.

Zilucoplan (RA101495) is a 15-amino acid cyclic peptide and an effective inhibitor of complement component 5 (C5). Zilucoplan can be used in research on immune-mediated necrotizing myopathy (IMNM).

Avacincaptad pegol (ARC1905) is an anti-C5 RNA aptamer that inhibits the cleavage of complement factor 5 (C5) into C5a and C5b.

NH2-C6-ARC186 sodium is a modified ARC186 with NH2-C6 that can be coupled to other peptides or molecules.