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The complement system helps or complementsthe 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
GY10564

LNP023

1644670-37-0

LNP023 (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.

GY06676

BR111

1037092-93-5

BR111 is a potent, highly selective and orally active antagonist of complement C3a receptor (C3aR) with IC50 of 85 ± 40  nM (inhibition of hC3a induced Ca2+ release on human macrophages); displays high selectivity for C3aR over C5aR; inhibits mast cell degranulation, thereby blocking recruitment and activation of macrophages and neutrophils, expression of inflammatory mediators and inflammation in a rat paw edema model.

GY06639

Avacopan

1346623-17-3

Avacopan (CCX-168, CCX168) is a potent, selective, orally availale C5aR (CD88) inhibitor with IC50 of 0.1 nM; shows no activity (IC50 >5,000 nM)for C5aR-related receptors C5L2, C3aR, ChemR23, GPR1 and FPR1; inhibits C5a-mediated chemotaxis of U937 cells with pA2 of 0.2 nM; shows activity in mouse model of ANCA-induced glomerulonephritis.

GY06629

Factor D inhibitor 6

1386455-51-1

Factor D inhibitor 6 is a potent and selective, orally bioavailable inhibitor of Factor D with IC50 of 30 nM; is highly selective for human FD, showing no inhibition of factor B; efficiently block alternative pathway activation and prevent both C3 deposition onto, and lysis of, PNH erythrocytes; inhibits lipopolysaccharide-induced AP activation in FD-humanized mice.

GY06628

Factor D inhibitor 7

1386455-76-0

Factor D inhibitor 7 is a potent and selective, orally bioavailable inhibitor of Factor D with IC50 of 50 nM; is highly selective for human FD, showing no inhibition of factor B; efficiently block alternative pathway activation and prevent both C3 deposition onto, and lysis of, PNH erythrocytes; inhibits lipopolysaccharide-induced AP activation in FD-humanized mice.

GY06624

BR103

1434873-26-3

BR103 is a potent, metabolically stable and highly selective small molecule agonist of complement C3a receptor (C3aR) with EC50 of 22 ± 8  nM; displays high selectivity for C3aR over C5aR; induces paw oedema and mast cell activation in vivo in rats.

GY06541

BCX-1470

217099-43-9

BCX-1470 is a serine protease inhibitor that inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM); displays 3.4-fold and 200-fold bette than that of trypsin, respectively; inhibits esterolytic activity translates into potent inhibition of the proteolytic activity of C1s, factor D, and consequently of the classical and alternative pathway-mediated hemolysis of target RBC (IC50=46 nM and 330 nM, respectively); blocks the reverse passive Arthus (RPA) reaction in rats.

GY06540

BCX-1470 methanesulfonate

217099-44-0

BCX-1470 methanesulfonate is a serine protease inhibitor that inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM); displays 3.4-fold and 200-fold bette than that of trypsin, respectively; inhibits esterolytic activity translates into potent inhibition of the proteolytic activity of C1s, factor D, and consequently of the classical and alternative pathway-mediated hemolysis of target RBC (IC50=46 nM and 330 nM, respectively); blocks the reverse passive Arthus (RPA) reaction in rats.

GY06538

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.

GY06565

Danicopan

1903768-17-1

Danicopan (ACH-4471, ACH-0144471) is a highly potent, orally active Factor D inhibitor with Kd of 0.54 nM, inhibits the proteolytic activity of purified Factor D against substrate Factor B in complex with C3b, blocking production of Bb fragment IC50 of 15 nM; significantly reduces complement-mediated hemolysis at concentrations as low as 10 nM in cells from paroxysmal nocturnal hemoglobinuria patients, decreases C3 fragment deposition on paroxysmal nocturnal hemoglobinuria erythrocytes; blocks alternative pathway activity when administered orally to cynomolgus monkeys.

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