1. Immunology/Inflammation
  2. Complement System

Avacopan (Synonyms: CCX168)

Cat. No.: HY-17627 Purity: 99.53% ee.: 99.54%
Handling Instructions

Avacopan (CCX168) is a potent, selective and orally available complement 5a receptor inhibitor with an IC50 of 0.1 nM.

For research use only. We do not sell to patients.

Avacopan Chemical Structure

Avacopan Chemical Structure

CAS No. : 1346623-17-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 154 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1008 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Avacopan (CCX168) is a potent, selective and orally available complement 5a receptor inhibitor with an IC50 of 0.1 nM.

IC50 & Target

IC50: 0.1 nM (complement 5a receptor )[1]

In Vitro

CCX168 displaces [125I]-C5a binding to C5aR on a human myeloid cell line (U937) with a potency (IC50) of 0.1 nM. CCX168 inhibits C5a-mediated chemotaxis of U937 cells with a potency (the concentration of CCX168 that produces a 2-fold right-shift in C5a activity) of 0.2 nM. CCX168 competitively and selectively blocked C5a-induced calcium mobilization in purified human neutrophils, with an IC50 value of 0.2 nM. CCX168 inhibited C5a-induced release of reactive-oxygen species from isolated neutrophils, and is able to completely block respiratory burst in these neutrophils[1].

In Vivo

CCX168 is shown to be well tolerated across a broad dose range (1 to 100 mg) and it showed dose-dependent pharmacokinetics. An oral dose of 30 mg CCX168 given twice daily blocked the C5a-induced upregulation of CD11b in circulating neutrophils by 94% or greater throughout the entire day, demonstrating essentially complete target coverage. In mice dosed orally with 0.03 mg/kg of CCX168, the resulting plasma CCX168 concentration of 15 nM (8.7 ng/mL) reduces the drop in circulating leukocytes from 53% to 25%. In mice administered 0.3 mg/kg of CCX168, the resulting plasma CCX168 concentration of 75 nM (44 ng/mL) reduces the drop in circulating leukocytes from 53% to only 10% relative to baseline (p<0.05 for CCX168 vs. vehicle control). Oral doses of CCX168 of either 3 or 30 mg/kg completely blocks C5a-induced leukopenia in hC5aR knock-in mice[1]. Oral CCX168, 30 mg/kg daily, reduces the severity of anti-MPO NCGN in hC5aR mice. Glomerular crescents are reduced from 30.4% to 3.3% with CCX168. Urine hematuria, proteinuria, and leukocyturia are reduced in mice receiving CCX168, 30 mg/kg per day. The protection by CCX168 results in reduced crescents and necrosis[2].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 10.1 mg/mL (17.36 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7193 mL 8.5964 mL 17.1928 mL
5 mM 0.3439 mL 1.7193 mL 3.4386 mL
10 mM 0.1719 mL 0.8596 mL 1.7193 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice: Human C5aR knock-in mice are dosed with vehicle (PEG-400/solutol-HS15 70:30, 5 mL/kg) or CCX168 by oral gavage. One hour after dosing, C5a (20 μg/kg, 0.1 mL dose volume) is injected intravenously and blood samples collected from retro-orbital eye bleeds. Blood leukocyte levels are analyzed by flow cytometry[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

581.64

Formula

C₃₃H₃₅F₄N₃O₂

CAS No.

1346623-17-3

SMILES

O=C([[email protected]@H]1[[email protected]](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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Avacopan
Cat. No.:
HY-17627
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Avacopan

Cat. No.: HY-17627