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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).
JPE-1375 (1 mg/kg; i.v.; single) demonstrates a rapid distribution in the plasma, followed by elimination in mice, and shows a strong negative correlation between PMN mobilization and TNF production with plasma concentrations.
| Molecular Weight | 955.08 |
| Formula | C49H63FN10O9 |
| CAS Number | 1254036-23-1 |
| Form | Solid |
| Solubility (25°C) | DMSO 96 mg/mL |
| Storage | 4°C, protect from light |
| Related Complement System Products |
|---|
| Eculizumab
Eculizumab is a first-in-class recombinant humanized monoclonal antibody targeting complement protein C5. C5, which can only recognize humans, cannot bind to C5 of other species. |
| 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. |
| 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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