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Cat. No. Product Name CAS No. Information
PC-35445

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.

Other Indication

Phase 2 Clinical

PC-61821

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.

PC-60253

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.

PC-60245

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.

Other Indication

Phase 3 Clinical

PC-45881

BCX-1470

217099-43-9

BCX-1470 (BCX1470) 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.

Thrombosis

Phase 1 Discontinued

PC-36148

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.

Other Indication

Phase 2 Clinical

PC-35224

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.

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