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MedKoo Cat#: 319575 | Name: Avacopan
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Avacopan, also known as CCX168, is an orally active, 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. CCX168 effectively blocked migration in in vitro and ex vivo chemotaxis assays, and it blocked the C5a-mediated neutrophil vascular endothelial margination. Avacopan was approved in 10/7/2021 for to treat severe active anti-neutrophil cytoplasmic autoantibody-associated vasculitis (granulomatosis with polyangiitis and microscopic polyangiitis) in combination with standard therapy, including glucocorticoids

Chemical Structure

Avacopan
Avacopan
CAS#1346623-17-3

Theoretical Analysis

MedKoo Cat#: 319575

Name: Avacopan

CAS#: 1346623-17-3

Chemical Formula: C33H35F4N3O2

Exact Mass: 581.2665

Molecular Weight: 581.66

Elemental Analysis: C, 68.14; H, 6.07; F, 13.07; N, 7.22; O, 5.50

Price and Availability

Size Price Availability Quantity
10mg USD 90.00 Ready to ship
25mg USD 190.00 Ready to ship
100mg USD 550.00 Ready to ship
200mg USD 950.00 Ready to Ship
500mg USD 1,650.00 Ready to ship
1g USD 2,950.00 Ready to ship
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Related CAS #
No Data
Synonym
Avacopan; CCX168; CCX-168; CCX 168.
IUPAC/Chemical Name
(2R,3S)-2-[4-(cyclopentylamino)phenyl]-1-(2-fluoro-6-methylbenzoyl)-N-[4-methyl-3-(trifluoromethyl)phenyl]piperidine-3-carboxamide
InChi Key
PUKBOVABABRILL-YZNIXAGQSA-N
InChi Code
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
SMILES Code
O=C([C@@H]1[C@H](C2=CC=C(NC3CCCC3)C=C2)N(C(C4=C(C)C=CC=C4F)=O)CCC1)NC5=CC=C(C)C(C(F)(F)F)=C5
Appearance
White to off-white solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 581.66 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Watanabe R, Hashimoto M. Perspectives of JAK Inhibitors for Large Vessel Vasculitis. Front Immunol. 2022 Mar 30;13:881705. doi: 10.3389/fimmu.2022.881705. PMID: 35432355; PMCID: PMC9005632. 2: Werion A, Rondeau E. Application of C5 inhibitors in glomerular diseases in 2021. Kidney Res Clin Pract. 2022 Mar 15. doi: 10.23876/j.krcp.21.248. Epub ahead of print. PMID: 35354244. 3: Gettman L. New Drugs Update: Finerenone, Difelikefalin, and Avacopan. Sr Care Pharm. 2022 Apr 1;37(4):130-138. doi: 10.4140/TCP.n.2022.130. PMID: 35337427. 4: Patel NJ, Stone JH. Expert Perspective: Management of ANCA-Associated Vasculitis. Arthritis Rheumatol. 2022 Mar 14. doi: 10.1002/art.42114. Epub ahead of print. PMID: 35289109. 5: van Leeuwen JR, Bredewold OW, van Dam LS, Werkman SL, Jonker JT, Geelhoed M, Langeveld APM, Remmelts HHF, van den Broecke MM, Ray A, Rabelink TJ, Teng YKO. Compassionate Use of Avacopan in Difficult-to-Treat Antineutrophil Cytoplasmic Antibody-Associated Vasculitis. Kidney Int Rep. 2021 Dec 8;7(3):624-628. doi: 10.1016/j.ekir.2021.11.036. PMID: 35257076; PMCID: PMC8897689. 6: Suresh E. The management of anti-neutrophil cytoplasmic antibody-associated vasculitis: what has changed in the last 10 years? Br J Hosp Med (Lond). 2022 Feb 2;83(2):1-10. doi: 10.12968/hmed.2021.0528. Epub 2022 Feb 23. PMID: 35243884. 7: Soulsby WD. Journal Club Review of "Avacopan for the Treatment of ANCA- Associated Vasculitis". ACR Open Rheumatol. 2022 Feb 15. doi: 10.1002/acr2.11412. Epub ahead of print. PMID: 35167187. 8: Ross C, Makhzoum JP, Pagnoux C. Updates in ANCA-associated vasculitis. Eur J Rheumatol. 2022 Feb 14. doi: 10.5152/eujrheum.2022.20248. Epub ahead of print. PMID: 35156630. 9: Arzoun H, Srinivasan M, Thangaraj SR, Thomas SS, Yarema A, Lee B, Mohammed L. Recent Advancements in the Management of Anti-neutrophil Cytoplasmic Antibody- Associated Vasculitis: A Systematic Review. Cureus. 2022 Feb 1;14(2):e21814. doi: 10.7759/cureus.21814. PMID: 35155037; PMCID: PMC8813156. 10: Holle JU, Hellmich B, Moosig F. Therapie-Update der ANCA-assoziierten Vaskulitiden: Granulomatose mit Polyangiitis und Mikroskopische Polyangiitis [Update on treatment of ANCA-associated vasculitis: Granulomatosis with polyangiitis and Microscopic Polyangiitis]. Z Rheumatol. 2022 Jan 21. German. doi: 10.1007/s00393-021-01154-5. Epub ahead of print. PMID: 35061059. 11: Koike H, Nishi R, Ohyama K, Morozumi S, Kawagashira Y, Furukawa S, Mouri N, Fukami Y, Iijima M, Sobue G, Katsuno M. ANCA-Associated Vasculitic Neuropathies: A Review. Neurol Ther. 2022 Mar;11(1):21-38. doi: 10.1007/s40120-021-00315-7. Epub 2022 Jan 19. PMID: 35044596; PMCID: PMC8857368. 12: Hellmich B, Henes JC. Biologika bei Kollagenosen und Vaskulitiden [Biologics for connective tissue diseases and vasculitides]. Internist (Berl). 2022 Feb;63(2):143-154. German. doi: 10.1007/s00108-021-01249-w. Epub 2022 Jan 14. PMID: 35029701. 13: Avacopan. Am J Health Syst Pharm. 2022 Feb 8;79(4):211-213. doi: 10.1093/ajhp/zxab438. PMID: 35024804. 14: Harigai M, Takada H. Avacopan, a selective C5a receptor antagonist, for anti-neutrophil cytoplasmic antibody-associated vasculitis. Mod Rheumatol. 2022 Apr 18;32(3):475-483. doi: 10.1093/mr/roab104. PMID: 34984461. 15: Muldur S, Vadysirisack DD, Ragunathan S, Tang Y, Ricardo A, Sayegh CE, Irimia D. Human Neutrophils Respond to Complement Activation and Inhibition in Microfluidic Devices. Front Immunol. 2021 Nov 24;12:777932. doi: 10.3389/fimmu.2021.777932. PMID: 34899737; PMCID: PMC8653703. 16: Freiwald T, Afzali B. Renal diseases and the role of complement: Linking complement to immune effector pathways and therapeutics. Adv Immunol. 2021;152:1-81. doi: 10.1016/bs.ai.2021.09.001. Epub 2021 Nov 19. PMID: 34844708; PMCID: PMC8905641. 17: Lee A. Avacopan: First Approval. Drugs. 2022 Jan;82(1):79-85. doi: 10.1007/s40265-021-01643-6. PMID: 34826105. 18: Moosig F, Holle JU. ANCA-assoziierte Vaskulitiden [ANCA-associated vasculitis]. Dtsch Med Wochenschr. 2021 Oct;146(19):1287-1290. German. doi: 10.1055/a-1308-5732. Epub 2021 Sep 22. PMID: 34553355. 19: Schönermarck U, Vielhauer V. Strategien zur effektiven und nebenwirkungsarmen Therapie ANCA-assoziierter Vaskulitiden [Strategies for effective treatment of ANCA-associated vasculitides with fewer side effects]. Nephrologe. 2021 Aug 30:1-12. German. doi: 10.1007/s11560-021-00527-w. Epub ahead of print. PMID: 34484454; PMCID: PMC8404175. 20: Koening CL, von Hennigs I. Antineutrophil cytoplasmic antibody (ANCA) vasculitis: pathophysiology, diagnosis, and the evolving treatment landscape. Am J Manag Care. 2021 Sep;27(15 Suppl):S267-S276. doi: 10.37765/ajmc.2021.88746. PMID: 34473462.