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Avacopan
🥰Excellent
Catalog No. T8223Cas No. 1346623-17-3
Alias CCX168
Avacopan (CCX168) is a C5aR antagonist (IC50=0.1 nM) with selective and oral activity. Avacopan blocks the action of C5a and prevents the development of GN induced by anti-myeloperoxidase antibodies in a mouse model of AAV. Avacopan can be used to treat anti-neutrophil cytoplasmic antibody (ANCA)-related vasculitis.
Avacopan
🥰Excellent
Purity: 99.9%
Catalog No. T8223Alias CCX168Cas No. 1346623-17-3
Avacopan (CCX168) is a C5aR antagonist (IC50=0.1 nM) with selective and oral activity. Avacopan blocks the action of C5a and prevents the development of GN induced by anti-myeloperoxidase antibodies in a mouse model of AAV. Avacopan can be used to treat anti-neutrophil cytoplasmic antibody (ANCA)-related vasculitis.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $33 | In Stock | |
| 5 mg | $83 | In Stock | |
| 10 mg | $133 | In Stock | |
| 25 mg | $282 | In Stock | |
| 50 mg | $448 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $126 | In Stock |
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Purity:99.9%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Avacopan (CCX168) is a C5aR antagonist (IC50=0.1 nM) with selective and oral activity. Avacopan blocks the action of C5a and prevents the development of GN induced by anti-myeloperoxidase antibodies in a mouse model of AAV. Avacopan can be used to treat anti-neutrophil cytoplasmic antibody (ANCA)-related vasculitis. |
| Targets&IC50 | C5aR:0.1 nM |
| In vitro | METHODS: MCF7 cell line was used for cytotoxicity, scratch assay, and flow cytometry analysis to validate the in vitro anti-tumor activity of Beta-Tetralone. RESULTS: Beta-Tetralone exhibited anticancer activity through dual targeting of MDM2 E3 ubiquitin ligase and Bcl-w anti-apoptotic protein.[1] METHODS: Beta-Tetralone biotransformation was monitored using KCh 6651 of Mycobacterium sp. at a substrate concentration of 1 g/L. RESULTS: Biotransformation of Beta-Tetralone yielded high yields of pure (S)-(-)-1,2,3,4-tetrahydro-2-naphthol.[2] |
| In vivo | CCX168 (avacopan), an orally administered selective and potent C5aR inhibitor.?CCX168 blocked the C5a binding, C5a-mediated migration, calcium mobilization, and CD11b upregulation in U937 cells as well as in freshly isolated human neutrophils.?CCX168 retains high potency when present in human blood.?A transgenic human C5aR knock-in mouse model allowed comparison of the in vitro and in vivo efficacy of the molecule.?CCX168 effectively blocked migration in in vitro and ex vivo chemotaxis assays, and it blocked the C5a-mediated neutrophil vascular endothelial margination.?CCX168 was effective in migration and neutrophil margination assays in cynomolgus monkeys[1]. |
| Alias | CCX168 |
| Molecular Weight | 581.64 |
| Formula | C33H35F4N3O2 |
| Cas No. | 1346623-17-3 |
| Smiles | C(=O)(N1[C@H]([C@@H](C(NC2=CC(C(F)(F)F)=C(C)C=C2)=O)CCC1)C3=CC=C(NC4CCCC4)C=C3)C5=C(C)C=CC=C5F |
| Relative Density. | 1.287 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
| Solubility Information | DMSO: 10 mg/mL (17.19 mM)  | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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