Complement System Inhibitor

Zaltenibart (OMS906) is an IgG4 humanized monoclonal antibody and MASP-3 inhibitor. By inhibiting MASP-3, Zaltenibart achieves upstream inhibition of the alternative complement pathway. MASP-3 is an upstream activator of Factor D (Factor D), a key enzyme in the alternative complement pathway. Zaltenibart prevents both intravascular hemolysis and extravascular hemolysis. Zaltenibart is applicable to research related to paroxysmal nocturnal hemoglobinuria.

Avacincaptad pegol (Izervay) is a selective inhibitor targeting complement component C5, and is a pegylated ribonucleic acid aptamer. Avacincaptad pegol inhibits the cleavage of C5 into pro-inflammatory C5a and C5b, which forms the membrane attack complex (C5b-9), thereby reducing inflammatory cell recruitment and retinal cell damage. Avacincaptad pegol can slow the growth of geographic atrophy (GA) lesions and reduce the risk of persistent vision loss. Avacincaptad pegol can be used in research of geographic atrophy associated with age-related macular degeneration (AMD) and has been approved by the FDA.

Dexamethasone-d₅ is the 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.

Zoracopan is a selective complement factor D (CFD) inhibitor. When administered systemically (orally or intravenously), Zoracopan accumulates and is sustained-released in ocular tissues, primarily in the choroid-retinal pigment epithelium (C-RPE) and/or iridociliary body (I-CB).

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.

Dexamethasone-d₃-1 (Hexadecadrol-d₃-1; Prednisolone F-d₃-1) is a deuterium labeled Dexamethasone (HY-14648). 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.

Olendalizumab (ALXN1007) is a mouse-derived and humanized IgG2-G4-κ antibody, targeting to Complement protein C5a (K_i=60 pM). Olendalizumab targets the complement inflammatory pathway. Moreover, Olendalizumab can be used for research of complement mediated disorder caused by corona virus.

ARC186 (sodium) is an unconjugated 40KDa PEG aptamer with a sequence identical to HY-147080 Avacincaptad pegol (ARC1905) sodium. ARC1905 is highly potent complement inhibitors that function by blocking the convertase-catalyzed activation of C5.

CP-289,503 is an inhibitor of the complement C5a receptor with an IC50 of 1 μM. C5a acts as an activator of leukocytes and phagocytes during complement system activation. The C5a receptor can bind to C5a, which can stimulate the upregulation of cell surface integrins and degranulation of inflammatory cells, leading to endothelial cell damage. C5a receptor inhibitors can block C5a signaling and inhibit a variety of inflammatory diseases.

ARC186 (sodium) is an unconjugated 40KDa PEG aptamer with a sequence identical to HY-147080 Avacincaptad pegol (ARC1905) sodium. ARC1905 is highly potent complement inhibitors that function by blocking the convertase-catalyzed activation of C5.

Cyclosporin A-¹³C₂,d₄ (Cyclosporine A-¹³C₂,d₄) is the deuterated, ¹³C-labeled Cyclosporin A (HY-B0579). 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.

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

Pexelizumab (h5G1. 1-SC) is a humanized scFv monoclonal antibody directed against the C5 complement component. Pexelizumab inhibits apoptosis and leukocyte infiltration. Pexelizumab can be used for the research of cerebral IR injury and myocardial infarction.

Cyclosporin A acetate-d₄ (Cyclosporine A acetate-d₄) is the deuterated-labeled Cyclosporin A (HY-B0579). 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.

NH2-C6-ARC186 sodium is a modified ARC186 (HY-153098) with NH₂-C₆ that can be coupled to other peptides or molecules. ARC186 is a aptamer and a highly potent complement inhibitor that function by blocking the convertase-catalyzed activation of C5.

HY-P990998 is an C5a-targeting IgG1κ type human antibody, the recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).

AKIR001 is a high-affinity human IgG1 antibody targeting CD44v6. AKIR001 carries LALA-silencing mutations in its FcγR-binding domain to reduce FcγR and C1q interactions, minimizing tissue interactions and limiting CDC and ADCC risks. [¹⁷⁷Lu] radiolabeled AKIR001, namely [¹⁷⁷Lu]Lu-AKIR001, has anticancer activity against epidermoid carcinoma.

SAR-443809 is a monoclonal antibody targeting complement factor Bb that inhibits the alternative complement pathway. SAR-443809 blocks the cleavage of C3 and factor B via selective binding to the activated form factor Bb, with a K_D of 7.3 nM for human factor Bb. SAR-443809 inhibits the amplification loop of the alternative complement pathway and C3 activation, reduces C3b deposition, and blocks the activation of pathways associated with intravascular and extravascular hemolysis. SAR-443809 can be used for research on hematological and renal disorders mediated by abnormal alternative complement pathway activity.

ANX-M1 Mouse IgG1 is a brain-penetrant C1q inhibitor. ANX-M1 Mouse IgG1 blocks classical complement pathway activation, reduces C1q concentrations in brain and plasma, and inhibits microglia-mediated synapse engulfment. ANX-M1 Mouse IgG1 can be used for the research of Huntington's disease, Alzheimer's disease, retinopathy and neuropathic pain.

Omoprubart is an anti-C5 complement recombinant humanized monoclonal antibody. Omolubat can prevent C5 from cleaving into C5a and C5b, thereby inhibiting the formation and activation of the C5b-dependent membrane attack complex (MAC) on the surface of susceptible cells, leading to cell lysis (destruction). Omoprubart can be used for the study of paroxysmal nocturnal hemoglobinuria (PNH).