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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Complement System Products |
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| P014
P014 is a C5 antibody/CFH fragment fusion protein that can be used in studies related to paroxysmal sleep hemoglobinuria (PNH) and thrombotic microangiopathy (TMA). |
| POT-4
POT-4 (AL-78898A), a Compstatin derivative, is a potent inhibitor of complement factor C3 activation. |
| TLQP-21
TLQP-21, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor 1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM). |
| N-((Allyloxy)carbonyl)-N-methyl-L-alanine
N-((Allyloxy)carbonyl)-N-methyl-L-alanine is a Alanine derivative. |
| C5a Receptor agonist, mouse, human
C5a Receptor agonist, mouse, human is a biological active peptide. |
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