2. Immunology/Inflammation
  3. Complement System
  4. Avacopan

Avacopan (CCX168) is a potent, selective and orally available complement 5a receptor (C5aR) inhibitor with an IC50 of 0.1 nM.

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

CAS No. : 1346623-17-3

Size Price Stock Quantity
Free Sample (0.1 - 0.2 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Avacopan:

Avacopan Related Antibodies

Top Publications Citing Use of Products
Microbiological Assay
Bio/Physico-chemical Assay
ELISA
Histological Imaging/Staining
WB
In Vivo Imaging

    Avacopan purchased from MedChemExpress. Usage Cited in: Neuron. 2025 Nov 18:S0896-6273(25)00803-7.  [Abstract]

    ELISA of iNOS, IL-1β, TNF-α, and IL-6 expression in TBI mice with or without Avacopan (30 mg/kg; p.o.; once daily for 7 days) administration (n = 6 mice/group). In TBI model, Avacopan significantly suppressed iNOS, IL-1β, TNF-α, and IL-6 expression.

    Avacopan purchased from MedChemExpress. Usage Cited in: Neuron. 2025 Nov 18:S0896-6273(25)00803-7.  [Abstract]

    Immunostaining and quantification of C3+ astrocytes of TBI mice with or without Avacopan (30 mg/kg; p.o.; once daily for 7 days) administration (n = 6 mice/group). Scale bar, 50 μm. The results showed that Avacopan significantly reduced C3+ astrocytes after TBI.

    Avacopan purchased from MedChemExpress. Usage Cited in: Neuron. 2025 Nov 18:S0896-6273(25)00803-7.  [Abstract]

    Relative expression of LGALS9 in TBI mice with or without Avacopan (30 mg/kg; p.o.; once daily for 7 days) treatment (n = 3 mice/group). The results showed that Avacopan significantly inhibited the expression of LGALS9

    Avacopan purchased from MedChemExpress. Usage Cited in: Neuron. 2025 Nov 18:S0896-6273(25)00803-7.  [Abstract]

    MRI imaging and analysis of injury volume, as well as cerebral edema assessments, in TBI mice with or without Avacopan (30 mg/kg; p.o.; once daily for 7 days) administered at 3 h and 3 days post-TBI (n = 6 mice/group). The results showed that Avacopan significantly reduced the severity of cerebral edema in TBI mice.

    Avacopan purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Oct 29.

    Inhibition of the C5a-induced response by the specific C5aR1 antagonist Avacopan. TNF-primed neutrophils were incubated without (solid line) or with Avacopan (50 nM, dashed line) for 5 min before addition of C5a (2 nM; added at the time point marked with an arrow) and determination of the NADPH oxidase activity. Inset: The inhibitory effect of Avacopan on the neutrophil NADPH oxidase activity expressed as peak values (Mcpm) of O2-production induced by C5a in absence and presence of the antagonist, respectively (mean ± SEM, n = 6).

    Avacopan purchased from MedChemExpress. Usage Cited in: Cell. 2023 Jun 22;186(13):2802-2822.e22.  [Abstract]

    Candida uptake by human neutrophils and killing by human macrophages (n=5–6). The results showed that Avacopan (500 nM; 30 min) decreased fungal uptake and killing by human neutrophils and macrophages, respectively.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Avacopan (CCX168) is a potent, selective and orally available complement 5a receptor (C5aR) 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].

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

    Avacopan Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    581.64

    Formula

    C33H35F4N3O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (171.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (4.30 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 98.50%

    SDS (536 KB)

    COA (252 KB) RP-HPLC (248 KB) MS (71 KB)

    Handling Instructions (2659 KB)
    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7193 mL 8.5964 mL 17.1928 mL 42.9819 mL
    5 mM 0.3439 mL 1.7193 mL 3.4386 mL 8.5964 mL
    10 mM 0.1719 mL 0.8596 mL 1.7193 mL 4.2982 mL
    15 mM 0.1146 mL 0.5731 mL 1.1462 mL 2.8655 mL
    20 mM 0.0860 mL 0.4298 mL 0.8596 mL 2.1491 mL
    25 mM 0.0688 mL 0.3439 mL 0.6877 mL 1.7193 mL
    30 mM 0.0573 mL 0.2865 mL 0.5731 mL 1.4327 mL
    40 mM 0.0430 mL 0.2149 mL 0.4298 mL 1.0745 mL
    50 mM 0.0344 mL 0.1719 mL 0.3439 mL 0.8596 mL
    60 mM 0.0287 mL 0.1433 mL 0.2865 mL 0.7164 mL
    80 mM 0.0215 mL 0.1075 mL 0.2149 mL 0.5373 mL
    100 mM 0.0172 mL 0.0860 mL 0.1719 mL 0.4298 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Avacopan Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Avacopan1346623-17-3CCX168CCX 168CCX-168Complement SystemInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Avacopan
    Cat. No.:
    HY-17627
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    English - EN (536 KB) Français - FR (536 KB) Deutsch - DE (536 KB) Norwegian - NO (536 KB) Español - ES (536 KB) Swedish - SV (536 KB) Italian - IT (536 KB) Korean - KR (536 KB) Portuguese - PT (536 KB)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.