Avacopan Inhibitor

Name: Avacopan Inhibitor; MyBioSource
Brand: MyBioSource
SKU: MBS5759036
Availability: InStock
Rating: 5 (10 reviews)

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5759036

Avacopan is an orally administered small-molecule C5aR ( IC50 : 0.1nM.)antagonist that blocks the effects of C5a and prevents the development of GN induced by anti-myeloperoxidase antibodies in a murine model of AAV. More details

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Product Documentation

Sample Manual Insert View PDF

Testing Data View PDF

Certificate of Analysis (COA) View PDF

QC Report View PDF

Material Safety Data Sheet View PDF

Technical Datasheet View PDF

Protocol View PDF

Product Overview

Online Datasheet in PDF

Product Name

Avacopan, Inhibitor

Full Product Name

Avacopan

Product Synonym Names

CCX168

Form/Format

Solid

Purity/Purification

99.9%

Preparation and Storage

Store at -20°C. Store at low temperature, keep away from direct sunlight.

Molecular Weight

581.60

Solubility

DMSO: 10.1mg/mL (17.36mM)
(<1mg/ml refers to the product slightly soluble or insoluble)

Formula

C33H35F4N3O2

CAS Number

1346623-17-3

Target & IC50

Complement System

HPLC

Consistent with structure

HNMR

Consistent with structure

Conclusion

The test result is consistent with structure.

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.

Preparing Stock Solution

1mg/5mg/10mg
1mM: (1mg) 1.7194, (5mg) 8.597, (10mg) 17.1939
5mM: (1mg) 0.3439, (5mg) 1.7194, (10mg) 3.4388
10mM: (1mg) 0.1719, (5mg)0.8597, (10mg) 1.7194
50mM: (1mg) 0.0344, (5mg) 0.1719, (10mg) 0.3439
Please select the appropriate solvent to prepare the stock solution, according to the solubility of the product in different solvents. Please use it as soon as possible.

Product Categories/Family for Avacopan, inhibitor

Immunology/Inflammation

Product References and Citations for Avacopan, inhibitor

Bekker P, et al. 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. 2016 Oct 21;11(10):e0164646.
Bekker P, et al. 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. 2016 Oct 21;11(10):e0164646.
Xiao H, et al. C5a receptor (CD88) blockade protects against MPO-ANCA GN. J Am Soc Nephrol. 2014 Feb;25(2):225-31.
Jayne D R W, Bruchfeld A N, Harper L, et al. Randomized Trial of C5a Receptor Inhibitor Avacopan in ANCA-Associated Vasculitis[J]. Journal of the American Society of Nephrology, 2017:ASN.2016111179.
Jayne D R W, Bruchfeld A N, Harper L, et al. Randomized Trial of C5a Receptor Inhibitor Avacopan in ANCA-Associated Vasculitis[J]. Journal of the American Society of Nephrology, 2017:ASN.2016111179.

Other Notes

Small volumes of Avacopan, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for Avacopan purchase

MBS5759036 is an inhibitor targeting Avacopan.