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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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| 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. |
| C5aR-IN-1
C5aR-IN-1 is a potent inhibitor of C5aR. |
| EG01377 dihydrochloride
EG01377 dihydrochloride is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of 609 nM for both NRP1-a1 and NRP1-b1. |
| Empasiprubart
Empasiprubar (ARGX-117) is a humanized inhibitory monoclonal antibody targeting complement C2. Empasiprubar binds to the Sushi-2 domain of C2, preventing the formation of C3 pre convertase and inhibiting the activation of classical and lectin pathways upstream of C3 activation. |
| Avacincaptad pegol sodium
Avacincaptad pegol (ARC1905) is an anti-C5 RNA aptamer that inhibits the cleavage of complement factor 5 (C5) into C5a and C5b. |
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