Complement System Inhibitor

Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist, apoptosis inducer, and common disease inducer in experimental animals, constructing models of muscle atrophy, hypertension, and depression. Dexamethasone can inhibit the production of inflammatory miRNA-155 exosomes in macrophages and significantly reduce the expression of inflammatory factors in neutrophils and monocytes. Dexamethasone also has potential for use in COVID-19 research.

Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC₅₀ of 5 nM. Cyclosporin A is a molecular glue, binds to cyclophilin and calcineurin, leading to inactivation of nuclear Factor of activated T Cells (NFAT) and a subsequent decrease in the immune response. Cyclosporin A also inhibits CD11a/CD18 adhesion.

Dextran sulfate sodium salt (DSS) (MW 5000) is a polymer of dehydrated glucose with a molecular weight of approximately 5000. Dextran sulfate sodium salt (DSS) with different molecular weights exhibits different biological activities. Dextran sulfate sodium salt (MW 5000) is an inhibitor of complement and coagulation pathways, and belongs to the glycosaminoglycans (GAG) family. Dextran sulfate sodium salt (MW 5000) acts as an anticoagulant, antiviral, and anti-lipemic agent. Dextran sulfate sodium salt (DSS) stops HIV-1 virus adsorption to host cells. Dextran sulfate sodium salt (MW 5000) prevents NK cell-mediated cytotoxicity. Dextran sulfate sodium salt (MW 5000) inhibits instant blood-mediated inflammatory reaction (IBMIR).

Iptacopan (LNP023) is an effective and orally-active highly selective factor B inhibitor with an IC₅₀ value of 10 nM and K_D of 7.9 nM. Iptacopan exerts a proximal effect in the complement cascade reaction, preventing the destruction (hemolysis) of red blood cells in PNH and the damage of renal cells in IgAN and C3G. Iptacopan can be used for the study of complement-mediated diseases, particularly paroxysmal nocturnal hemoglobinuria (PNH), primary immunoglobulin A nephropathy (IgAN), and complement 3 glomerulopathy (C3G).

Lexucitug (DCSZ-11) is a humanized monoclonal antibody targeting CD93. The antibody isotype of Lexucitug is human IgG1κ; the recommended isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).

Ascuprubart is an anti-human monoclonal antibody targeting Complement C5.

NRPa-308 is a potent and orally active Neuropilin-1 (NRP-1) antagonist with an IC₅₀ of 42 μM for inhibiting VEGF-A₁₆₅ binding to NRP-1. NRPa-308 blocks the specific interaction between VEGF-A₁₆₅ and NRP-1. NRPa-308 effectively suppresses angiogenesis in vitro and in vivo and reduces the viability of a broad spectrum of human solid and haematological cancer cells. NRPa-308 inhibits tumor growth and prolongs median survival in a human breast cancer xenograft mouse model. NRPa-308 can be used for the research of multiple human malignancies including solid tumors and hematological cancers.

Dexamethasone (Hexadecadrol) Water Soluble is a water-soluble form of Dexamethasone (HY-14648). Dexamethasone is a glucocorticoid receptor agonist, apoptosis inducer, and a common disease inducer in experimental animals. It can be used to construct models of muscle atrophy, hypertension, and depression. Dexamethasone can inhibit the production of inflammatory miRNA-155 exosomes in macrophages and significantly reduce the expression of inflammatory factors in neutrophils and monocytes. Dexamethasone also has the potential to be used in COVID-19 research.(Sale size is the weight of dexamethasone)

Pegcetacoplan acetate is a pegylated complement C3/C3b inhibitor. Pegcetacoplan acetate acts by specifically binding to and inhibiting C3 and C3b, thereby suppressing the complement cascade at its proximal stage. Pegcetacoplan is not a known inhibitor or inducer of CYP450 isoenzymes. Pegcetacoplan acetate can be used for the research of complement-mediated diseases, including paroxysmal nocturnal hemoglobinuria (PNH) and age-related macular degeneration (AMD).

Avacopan (CCX168) is a potent, selective and orally available complement 5a receptor (C5aR) inhibitor with an IC₅₀ of 0.1 nM.

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 inhibits deployment of the terminal complement system including the formation of membrane attack complex (MAC). Eculizumab prevents anti-ganglioside antibody-mediated neuropathy in mice. Eculizumab can be used in hemolysis studies.

Danicopan (ACH-4471), a selective and orally active small-molecule factor D inhibitor, shows high binding affinity to human Factor D with K_d value of 0.54 nM. Danicopan (ACH-4471) inhibits alternative pathway of complement (APC) activity, has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS).

Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates’ complement system. Compstatin exhibits IC₅₀ values of 63 μM and 12 μM for classical and alterative complement pathway, respectively.

Tanruprubart (ANX005) is a C1q inhibitor and C1q depleter. Tanruprubart is a human antibody expressed in CHO cells, with huIgG1 heavy chains and huκ light chains, and its predicted molecular weight (MW) is 145 kDa. For the isotype control of Tanruprubart, refer to Human IgG4 kappa, Isotype Control (HY-P99003). The IC₅₀ of Tanruprubart is 346 ng/mL for humans and 259 ng/mL for rats; its EC₅₀ is 3.8 ng/mL for humans, 5.2 ng/mL for rats, and 9.9 ng/mL for mice. Tanruprubart is applicable to the research of Guillain-Barré syndrome and Alzheimer's disease.

Avacincaptad pegol (ARC1905) sodium is a 40KDa PEG-conjugated aptamer. Avacincaptad pegol sodium targets complement factor 5 (C5), inhibits the cleavage of C5 into C5a and C5b, limits inflammatory stimulation and complement membrane attack complex (MAC), and is used to study age-related macular degeneration (AMD). Avacincaptad pegol sodium limits irregular cell apoptosis by targeting downstream factors in the complement cascade while preserving the early steps of the complement system.

Sutimlimab is a humanized monoclonal IgG4 antibody. Sutimlimab inhibits complement protein component 1, s subcomponent (C1s). Sutimlimab blocks C3 and C4 activation. Sutimlimab can be used for the research of cold agglutinin disease and complement-mediated hemolytic uremic syndrome.

AMY-101 TFA (Cp40 TFA), a peptidic inhibitor of the central complement component C3 (K_D = 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.

AMY-101 (Cp40), a peptidic inhibitor of the central complement component C3 (K_D = 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.

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

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.