Complement System

LNP023 is a highly potent factor B (FB) inhibitor with an IC50 value of 10 nM. LNP023 shows direct, reversible, and high-affinity binding to human FB (KD=7.9 nM).

Complement factor D-IN-1 is a potent and selective small-molecule reversible factor d inhibitor, with IC50s of 0.006 and 0.05 μM in FD Thioesterolytic Fluorescent Assay and a MAC Deposition Assay, respectively.

Danicopan (ACH-4471), a selective and orally active small-molecule factor D inhibitor, shows high binding affinity to human Factor D with Kd value of 0.54 nM.

Complement C5-IN-1 (Compound 7) is a small-molecule inhibitor of complement component 5 protein (C5).

3-Phenoxybenzaldehyde is a compound identified as a complement inhibitor, exhibiting weak inhibition of the classical pathway of the complement system. This compound demonstrates hemolytic activity, making it relevant for studies related to immune response modulation and complement pathway research. Its applications extend to investigations in autoimmune diseases and therapies targeting complement-mediated cytotoxicity.

Avacincaptad pegol is a pegylated RNA aptamer that selectively inhibits complement component C5. By preventing the cleavage of C5 into pro-inflammatory fragments C5a and C5b, this compound mitigates inflammatory cell recruitment and reduces retinal cell damage. Avacincaptad pegol has demonstrated potential in slowing the progression of geographic atrophy (GA) lesions and decreasing the risk of vision loss, making it a valuable tool for research involving age-related macular degeneration (AMD).

Factor B-IN-1 is an inhibitor of Factor B, targeting the complement system to modulate its activity. This compound demonstrates significant inhibition of the alternative pathway of complement activation, making it a valuable tool for studying complement-mediated diseases and immune responses. Factor B-IN-1 is suitable for use in research applications focused on therapeutic interventions and the development of complement-targeted therapies.

Complement Factor D-IN-2 is an inhibitor targeting complement factor D, effectively interrupting the complement cascade at a critical juncture within the alternative complement pathway. By inhibiting factor D, this compound presents valuable opportunities for investigating the role of complement activation in autoimmune diseases. Researchers can utilize Complement Factor D-IN-2 to explore therapeutic strategies aimed at modulating immune responses and mitigating the progression of complement-mediated pathologies.

Refinicopan is a selective inhibitor of complement factor D, demonstrating an IC50 of 10 nM. This compound effectively inhibits rabbit erythrocyte hemolysis with an IC50 of 41 nM, indicating its capacity to modulate complement-mediated processes. Refinicopan's favorable pharmacokinetic and pharmacodynamic properties make it a valuable tool for investigating complement-related disorders and potential therapeutic interventions.

Vensobafusp alfa is a fusion protein that targets complement protein C5, functioning as a potent inhibitor. It combines an IgG4 monoclonal antibody directed against C5 with the complement factor H 1-5 domain, demonstrating significant anti-inflammatory and immunomodulatory properties. This reagent is applicable in the study of complement-mediated pathologies and therapeutic strategies targeting inflammatory conditions.

Bisphenol A bissulfate disodium is a complement system inhibitor with a significant role in modulating immune responses. This compound exhibits complement-inhibiting activity, demonstrating an IC50 value of 247 μM. It is utilized in research applications aimed at understanding the complement pathway and its implications in various diseases, making it a valuable tool in immunological studies.

Bisphenol S disulfate disodium is a complement inhibitor that exhibits a half-maximal inhibitory concentration (IC50) of 660 μM. This compound is utilized in research applications aiming to explore complement-mediated pathways and their roles in various biological processes and diseases. Its ability to modulate complement activity makes it a valuable tool for studies involving immune response and inflammation.

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.

POT-4 (AL-78898A), a Compstatin derivative, is a potent inhibitor of complement factor C3 activation. POT-4 can be used for age-related macular degeneration research

Dextran sulfate sodium salt (DSS, MW 5000) primarily functions as a complement inhibitor, derived from a polymer of dehydrated glucose. This compound exhibits significant biological activities, including anticoagulation, antiviral properties, and anti-lipemic effects. Its mechanisms involve blocking HIV-1 adsorption to host cells, preventing natural killer (NK) cell-mediated cytotoxicity, and inhibiting instant blood-mediated inflammatory reactions (IBMIR). Dextran sulfate sodium salt (MW 5000) is valuable in research related to immunology, virology, and cardiovascular studies.

EG01377 dihydrochloride is a potent, bioavailable, and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM and IC₅₀ values of 609 nM for both NRP1-a1 and NRP1-b1 domains. It exhibits antiangiogenic, antimigratory, and antitumor activities.

Perforin-IN-2 (Compound 1) is a perforin inhibitor that blocks perforin-mediated cell lysis. It has potential to reduce graft rejection in the context of allogeneic bone marrow or stem cell transplantation.

Vemircopan (ALXN2050) is an orally active inhibitor of complement factor D (FD). It is being investigated for the treatment of complement-mediated diseases, including myasthenia gravis, lupus nephritis, IgA nephropathy, and paroxysmal nocturnal hemoglobinuria (PNH).

Pelecopan (BCX9930) is a potent, selective, and orally active inhibitor of complement factor D, with an IC₅₀ value of 14.3 nM. It targets factor D to prevent both intravascular and extravascular hemolysis in paroxysmal nocturnal hemoglobinuria (PNH) and is also applicable to other diseases mediated by the alternative complement pathway.

Zoracopan is a selective inhibitor of complement factor D (CFD). Upon systemic administration (oral or intravenous), it preferentially accumulates in ocular tissues and is released in a sustained manner, primarily targeting the choroid–retinal pigment epithelium (C-RPE) and/or iridociliary body (I-CB).

PIC1 PA is a 15-amino-acid peptide and a potent analog of PIC1 that inhibits classical pathway–mediated complement activation. It functions by disrupting the interaction between C1s-C1r-C1r-C1s/MASPs and the collagen-like region (CLR) of C1q or MBL. PIC1 PA specifically binds to the CLR of C1q, with a mean equilibrium dissociation constant (K\_D) of 33.3 nM for purified C1q.

Tarvicopan is an inhibitor for complement factor D.

Lanoracopan is a potent inhibitor of complement factor B, with an IC₅₀ of 1.2 μM. It is suitable for research in inflammation- and immunity-related diseases.

CP-289,503 is an inhibitor of the complement C5a receptor, with an IC₅₀ of 1 μM. The C5a receptor mediates pro-inflammatory signaling by binding to C5a, a complement activation product that stimulates leukocyte and phagocyte activation, upregulates integrins, and induces degranulation of inflammatory cells, contributing to endothelial damage. By blocking C5a signaling, CP-289,503 may be useful in the treatment of various inflammatory diseases.