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SKU | Size | Availability | Price | Qty |
---|---|---|---|---|
A607815-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,334.90 | |
A607815-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $2,001.90 |
Synonyms | (2R,3S)-2-[4-(Cyclopentylamino)phenyl]-1-(2-fluoro-6-methylbenzoyl)-N-[4-methyl-3-(trifluoromethyl)phenyl]-3-piperidinecarboxamide | AVACOPAN [WHO-DD] | CCX168 | CCX-168 | GTPL9450 | Tavneos | Avacopan [USAN] | avacopanum | (2R,3S)-2-[4-(cyclopentylamino) |
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Specifications & Purity | Moligand™ |
Grade | Moligand™ |
Action Type | ANTAGONIST |
Mechanism of action | C5a anaphylatoxin chemotactic receptor antagonist |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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IUPAC Name | (2R,3S)-2-[4-(cyclopentylamino)phenyl]-1-(2-fluoro-6-methylbenzoyl)-N-[4-methyl-3-(trifluoromethyl)phenyl]piperidine-3-carboxamide |
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INCHI | InChI=1S/C33H35F4N3O2/c1-20-12-15-25(19-27(20)33(35,36)37)39-31(41)26-10-6-18-40(32(42)29-21(2)7-5-11-28(29)34)30(26)22-13-16-24(17-14-22)38-23-8-3-4-9-23/h5,7,11-17,19,23,26,30,38H,3-4,6,8-10,18H2,1-2H3,(H,39,41)/t26-,30-/m0/s1 |
InChi Key | PUKBOVABABRILL-YZNIXAGQSA-N |
Canonical SMILES | O=C([C@H]1CCCN([C@H]1c1ccc(cc1)NC1CCCC1)C(=O)c1c(C)cccc1F)Nc1ccc(c(c1)C(F)(F)F)C |
Isomeric SMILES | CC1=C(C(=CC=C1)F)C(=O)N2CCC[C@@H]([C@@H]2C3=CC=C(C=C3)NC4CCCC4)C(=O)NC5=CC(=C(C=C5)C)C(F)(F)F |
PubChem CID | 49841217 |
1. Bekker P, Dairaghi D, Seitz L, Leleti M, Wang Y, Ertl L, Baumgart T, Shugarts S, Lohr L, Dang T et al.. (2016) Characterization of Pharmacologic and Pharmacokinetic Properties of CCX168, a Potent and Selective Orally Administered Complement 5a Receptor Inhibitor, Based on Preclinical Evaluation and Randomized Phase 1 Clinical Study.. PLoS ONE, 11 (10): (e0164646). [PMID:27768695] [10.1021/op500134e] |
2. Jayne DRW, Bruchfeld AN, Harper L, Schaier M, Venning MC, Hamilton P, Burst V, Grundmann F, Jadoul M, Szombati I et al.. (2017) Randomized Trial of C5a Receptor Inhibitor Avacopan in ANCA-Associated Vasculitis.. J Am Soc Nephrol, 28 (9): (2756-2767). [PMID:28400446] [10.1021/op500134e] |
3. Kettritz R. (2017) Vasculitis: A CLEAR argument for targeting complement in ANCA vasculitis.. Nat Rev Nephrol, 13 (8): (448-450). [PMID:28529340] [10.1021/op500134e] |
4. Merkel PA, Jayne DR, Wang C, Hillson J, Bekker P. (2020) Evaluation of the Safety and Efficacy of Avacopan, a C5a Receptor Inhibitor, in Patients With Antineutrophil Cytoplasmic Antibody-Associated Vasculitis Treated Concomitantly With Rituximab or Cyclophosphamide/Azathioprine: Protocol for a Randomized, Double-Blind, Active-Controlled, Phase 3 Trial.. JMIR Res Protoc, 9 (4): (e16664). [PMID:32088663] [10.1021/op500134e] |
5. Serling-Boyd N, Wallace ZS. (2021) Management of primary vasculitides with biologic and novel small molecule medications.. Curr Opin Rheumatol, 33 (1): (8-14). [PMID:33164993] [10.1021/op500134e] |
6. Onuora S. (2021) Avacopan offers alternative to steroids for ANCA-associated vasculitis.. Nat Rev Rheumatol, 17 (5): (249). [PMID:33846585] [10.1021/op500134e] |
7. Osman M, Cohen Tervaert JW, Pagnoux C. (2021) Avacopan for the treatment of ANCA-associated vasculitis.. Expert Rev Clin Immunol, 17 (7): (717-726). [PMID:34006155] [10.1021/op500134e] |
8. Horiuchi T, Tsukamoto H. (2016) Complement-targeted therapy: development of C5- and C5a-targeted inhibition.. Inflamm Regen, 36 (13): (11). [PMID:29259684] [10.1021/op500134e] |
9. Jayne D. (2019) Complement inhibition in ANCA vasculitis.. Nephrol Ther, 15 (6): (409-412). [PMID:31631015] [10.1021/op500134e] |