All AbMole products are for research use only, cannot be used for human consumption.
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.
Avacopan (CCX168) blocked the C5a binding, C5a-mediated migration, calcium mobilization, and CD11b upregulation in U937 cells as well as in freshly isolated human neutrophils. Avacopan competitively and selectively blocked C5a-induced calcium mobilization in purified human neutrophils, with an IC50 value of 0.2 nM.
In vivo, in mice dosed orally with 0.03 mg/kg of CCX168, the resulting plasma CCX168 concentration of 15 nM (8.7 ng/mL) reduces the drop in circulating leukocytes from 53% to 25%. In mice administered 0.3 mg/kg of CCX168, the resulting plasma CCX168 concentration of 75 nM (44 ng/mL) reduces the drop in circulating leukocytes from 53% to only 10% relative to baseline (p<0.05 for CCX168 vs. vehicle control). Oral doses of CCX168 of either 3 or 30 mg/kg completely blocks C5a-induced leukopenia in hC5aR knock-in mice.
Exp Ther Med. 2022 Jun 7;24(2):493.
The complement C3a-C3aR and C5a-C5aR pathways promote viability and inflammation of human retinal pigment epithelium cells by targeting NF-κB signaling
Avacopan purchased from AbMole
| Molecular Weight | 581.64 |
| Formula | C33H35F4N3O2 |
| CAS Number | 1346623-17-3 |
| Solubility (25°C) | DMSO ≥ 9 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Xiao H, et al. J Am Soc Nephrol. C5a receptor (CD88) blockade protects against MPO-ANCA GN.
| Related Complement System Products |
|---|
| 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. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
