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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-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.
PC-62226

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.
PC-62225

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.
PC-61772

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.

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