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avacopan , C5a anaphylatoxin chemotactic receptor antagonist, CAS No.A607815, C5a anaphylatoxin chemotactic receptor antagonist

Item Number
A607815
Grouped product items
SKUSizeAvailabilityPrice 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

Basic Description

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)
Specifications & PurityMoligand™
GradeMoligand™
Action TypeANTAGONIST
Mechanism of actionC5a anaphylatoxin chemotactic receptor antagonist

Associated Targets(Human)

C5AR1 Tclin C5a anaphylatoxin chemotactic receptor 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Associated Targets(non-human)

rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Names and Identifiers

IUPAC Name (2R,3S)-2-[4-(cyclopentylamino)phenyl]-1-(2-fluoro-6-methylbenzoyl)-N-[4-methyl-3-(trifluoromethyl)phenyl]piperidine-3-carboxamide
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

Certificates

C of A & Other Certificates

Related Documents

References

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,  (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]

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