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Eculizumab is also monospecific for human C5, and does not bind to C5 from other species, including the mouse.
Eculizumab is a first-in-class recombinant humanized monoclonal antibody targeting complement protein C5.It is an immunoglobulin G-kappa (IgGκ) consisting of human constant regions and murine complementarity-determining regions grafted onto human framework light and heavy chain variable regions.
Eculizumab specifically binds to the terminal complement component 5, or C5, which acts at a late stage in the complement cascade. When activated, C5 is involved in activating host cells, thereby attracting pro-inflammatory immune cells, while also destroying cells by triggering pore formation. By inhibiting the complement cascade at this point, the normal, disease-preventing functions of proximal complement system are largely preserved, while the properties of C5 that promote inflammation and cell destruction are impeded.
Eculizumab inhibits the cleavage of C5 by the C5 convertase into C5a a potent anaphylatoxin with prothrombotic and proinflammatory properties, and C5b, which then forms the terminal complement complex C5b-9 which also has prothrombotic and proinflammatory effects. Both C5a and C5b-9 cause the complement-mediated events that are characteristic of PNH and aHUS.
| Molecular Weight | 148000.0 |
| CAS Number | 219685-50-4 |
| Storage | -80°C for long term |
| Related Complement System Products |
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| SB290157 trifluoroacetate salt
SB290157 is a selective antagonist of complement anaphylatoxin C3a receptor, a 74 amino acid proinflammatory peptide that is a potent chemotaxin for eosinophils, macrophages and mast cells. |
| JPE-1375
JPE-1375 is a complement C5a receptor 1 (C5aR1) antagonist. JPE-1375 effectively inhibits polymorphonuclear leukocyte mobilization (EC50=6.9 µM) and reduces TNF levels (EC50=4.5 µM) in mice. |
| Compstatin
Compstatinis is a 13-residue cyclic peptide, binds to complement component C3 and inhibits complement activation with IC50 of 12 μM. Compstatin exhibits exclusive specificity for primate C3s and does not bind either to C3s from lower mammalian species or to two structural homologs of C3, human C4 and C5. |
| Avacopan
Avacopan (CCX168) is a first-in-class, potent, selective and orally available complement 5a receptor (C5aR1 or CD88) antagonist with an IC50 of 0.1 nM. |
| AMY-101 acetate
AMY-101 acetate is a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM). |
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