Avacopan | CAS#1346623-17-3 | C5aR inhibitor| MedKoo

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

MedKoo CAT#: 319575

CAS#: 1346623-17-3

Description: 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

CAS# 1346623-17-3

Instruction

Theoretical Analysis

MedKoo Cat#: 319575
Name: Avacopan
CAS#: 1346623-17-3
Chemical Formula: C33H35F4N3O2
Exact Mass: 581.27
Molecular Weight: 581.660
Elemental Analysis: C, 68.14; H, 6.07; F, 13.07; N, 7.22; O, 5.50

Price and Availability

Size	Price	Availability
10mg	USD 90	Ready to ship
25mg	USD 190	Ready to ship
100mg	USD 550	Ready to ship
200mg	USD 950	Ready to Ship
500mg	USD 1650	Ready to ship
1g	USD 2950	Ready to ship
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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:

Certificate of Analysis:

View CoA: current batch, Lot#Y7X06M09

QC Data:

View QC data: current batch, Lot#Y7X06M09

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

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.

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

Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.

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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.

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