Complement System|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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The complement system helps or “complements” the ability of antibodies and phagocytic cells to clear pathogens from an organism. It is part of the immune system called the innate immune system that is not adaptable and does not change over the course of an individual's lifetime. The complement system consists of a number of small proteins found in the blood, in general synthesized by the liver, and normally circulating as inactive precursors (pro-proteins). When stimulated by one of several triggers, proteases in the system cleave specific proteins to release cytokines and initiate an amplifying cascade of further cleavages. The end-result of this activation cascade is massive amplification of the response and activation of the cell-killing membrane attack complex. Over 30 proteins and protein fragments make up the complement system. Three biochemical pathways activate the complement system: the classical complement pathway, the alternative complement pathway, and the lectin pathway.

Cat. No.	Product Name	CAS No.	Information
H9358	Vemircopan	2086178-00-7	Vemircopan is a potent,oral the second-generation Factor D inhibitor.
H9218	AMY-101 TFA	1789738-04-0	AMY-101 TFA (Cp40 TFA), 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.
H9217	AMY-101	1427001-89-5	AMY-101 is 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.
H8748	Lonodelestat	906547-89-5	Lonodelestat is a protease inhibitor.
H3959	W-54011	405098-33-1	A potent and orally active non-peptide C5a receptor (CD88;C5aR) antagonist with Ki of 2.2 nM; also inhibits C5a-induced intracellular Ca(2+) mobilization, chemotaxis, and generation of reactive super oxide species in human neutrophils with IC50 of 3.1, 2.7, and 1.6 nM, respectively; inhibits C5a-induced neutropenia in gerbils (3-30 mg/kg).
H3958	SB 290157	259218-28-5	A potent, selective nonpeptide antagonist of anaphylatoxin C3a receptor (C3aR) with IC50 of 200 nM; does not antagonize the C5aR or 5 other chemotactic GPCRs on human neutrophils; blocks C3a-induced C3aR internalization and C3a-induced Ca(2+) mobilization in RBL-C3aR cells and human neutrophils with IC50 of 27.7 and 28 nM, respectively; also inhibits C3a-induced Ca2+ mobilization of mouse and guinea pig C3aRS with IC50 of 7 and 12.5 nM, respectively; potently inhibits C3a-mediated ATP release from guinea pig platelets and inhibits C3a-induced potentiation of the contractile response to field stimulation of perfused rat caudal artery, demonstrates antiinflammatory activity in animal models.
H3957	PMX53	219639-75-5	PMX53 (Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg)) is a potent C5a receptor (CD88) antagonist with IC50 of 20 nM, also is an agonist for Mas-related gene 2 (MrgX2) in human mast cells; PMX-53 (10 nM) inhibited C5a-induced Ca(2+) mobilization in HMC-1 cells, but at higher concentrations (>30 nM) it caused degranulation in LAD2 mast cells, CD34(+) cell-derived mast cells, and RBL-2H3 cells stably expressing MrgX2; inhibits zymosan-, carrageenan-, LPS- and antigen-induced hypernociception in rats.
H3956	NDT 9513727	439571-48-9	NDT 9513727 is a potent, selective and orally bioavailable C5a receptor inverse agonist with IC50 of 11.6 nM in radioligand binding assay; exhibits potent activity in both gerbil and monkey lung membrane preparations (6.4 and 7.3 nM), but has minimal activity in rat, mouse, and dog lung preparations (>10 uM); blocks hC5a-stimulated chemotaxis activity in human polymorphonuclear neutrophils and U937 cells with IC50 of 4.7 and 4.3 nM, respectively, inhibits C5a-stimulated responses, including guanosine 5'-3-O-(thio)triphosphate binding, Ca(2+) mobilization, oxidative burst, degranulation, cell surface CD11b expression and chemotaxis in various cell types with IC50 of 1.1-9.2 nM; effectively inhibits C5a-induced neutropenia in gerbil and cynomolgus macaque in vivo.
H3955	LNP023	1644670-37-0	Iptacopan (LNP-023) is a highly potent, reversible, selective inhibitor of factor B (IC50=10 nM), the proteolytically active component of the C3 and C5 convertases; shows direct, reversible, and high-affinity binding to human FB with Kd of 7.9 nM in SPR assays, demonstrates potent inhibition of AP-induced MAC formation in 50% human serum with IC50 of 0.13 uM; shows no inhibition of factor D (FD), as well as classical or lectin complement pathway activation (up to 100 uM), and no significant effects (up to 10 μM) in a broad assay panel of receptors, ion channels, kinases, and proteases; blocks zymosan-induced MAC formation membrane attack complex (MAC) with IC50 of 0.15 uM, prevents KRN-induced arthritis in mice and is effective upon prophylactic and therapeutic dosing in an experimental model of membranous nephropathy in rats afer oral adminstration; also prevents complement activation in sera from C3 glomerulopathy patients and the hemolysis of human PNH erythrocytes.
H3954	Leukadherin 1	344897-95-6	Leukadherin 1 (LA1) is a small molecule allosteric agonist of integrin CD11b/CD18 (CR3), increases CD11b/CD18-dependent cell adhesion to fibrinogen (EC50=4 uM); reduces IFN-I responses in WT but not CD11b-deficient mice, and protects lupus-prone MRL/Lpr mice from end-organ injury; reduces TLR-dependent proinflammatory signaling in leukocytes and suppresses IFN-I signaling via an AKT/FOXO3/IFN regulatory factor 3/7 pathway.

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