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

Danicopan (ACH-4471), a selective and orally active small-molecule factor D inhibitor, shows high binding affinity to human Factor D with Kd value of 0.54 nM. Danicopan (ACH-4471) inhibits alternative pathway of complement (APC) activity, has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS).

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

CAS No. : 1903768-17-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Danicopan Related Antibodies

Top Publications Citing Use of Products

    Danicopan purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2022 Jan 8;14(2):305.

    cSCC cell cultures (UT-SCC-12A) were treated with a small-molecule factor D inhibitor (danicopan; ACH-4471) or DMSO as vehicle control for 24 h. The levels of complement factor B (FB) and its 60 kDa cleavage derivative in conditioned media of cSCC cells were determined by Western blot analysis.

    Danicopan purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2022 Jan 8;14(2):305.

    cSCC cells (UT-SCC-12A) with high basal FD expression levels were treated with small molecule FD inhibitors (danicopan; ACH-4471) or DMSO. Targeted inhibition of FD significantly suppressed cell proliferation.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Danicopan (ACH-4471), a selective and orally active small-molecule factor D inhibitor, shows high binding affinity to human Factor D with Kd value of 0.54 nM. Danicopan (ACH-4471) inhibits alternative pathway of complement (APC) activity, has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS)[1].

    IC50 & Target

    Kd: 0.54 nM (Factor D)[1]
    In Vitro

    Danicopan (ACH-4471) inhibits the proteolytic activity of purified Factor D against its natural substrate Factor B in complex with C3b, blocking production of Bb fragment in a dose-dependent manner with an IC50 value of 0.015 μM[1].
    Danicopan (ACH-4471) potently inhibits hemolysis with IC50 values ranging from 0.0040 μM to 0.027 μM (IC90 values from 0.015 μM to 0.11 μM)[1].

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

    Danicopan Related Antibodies
    Clinical Trial
    Molecular Weight

    580.41

    Formula

    C26H23BrFN7O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C([C@H]1N(C(CN2N=C(C(C)=O)C3=C2C=CC(C4=CN=C(C)N=C4)=C3)=O)C[C@H](F)C1)NC5=NC(Br)=CC=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 : 125 mg/mL (215.37 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 1.7229 mL 8.6146 mL 17.2292 mL
    5 mM 0.3446 mL 1.7229 mL 3.4458 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: ≥ 2.08 mg/mL (3.58 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    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: 99.91%

    SDS (393 KB)

    COA (253 KB) HNMR (344 KB) RP-HPLC (122 KB) LCMS (121 KB)

    Handling Instructions (2659 KB)
    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 1.7229 mL 8.6146 mL 17.2292 mL 43.0730 mL
    5 mM 0.3446 mL 1.7229 mL 3.4458 mL 8.6146 mL
    10 mM 0.1723 mL 0.8615 mL 1.7229 mL 4.3073 mL
    15 mM 0.1149 mL 0.5743 mL 1.1486 mL 2.8715 mL
    20 mM 0.0861 mL 0.4307 mL 0.8615 mL 2.1537 mL
    25 mM 0.0689 mL 0.3446 mL 0.6892 mL 1.7229 mL
    30 mM 0.0574 mL 0.2872 mL 0.5743 mL 1.4358 mL
    40 mM 0.0431 mL 0.2154 mL 0.4307 mL 1.0768 mL
    50 mM 0.0345 mL 0.1723 mL 0.3446 mL 0.8615 mL
    60 mM 0.0287 mL 0.1436 mL 0.2872 mL 0.7179 mL
    80 mM 0.0215 mL 0.1077 mL 0.2154 mL 0.5384 mL
    100 mM 0.0172 mL 0.0861 mL 0.1723 mL 0.4307 mL
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    Danicopan 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:

    Danicopan1903768-17-1ACH-4471ACH4471ACH 4471Complement SystemInhibitorinhibitorinhibit

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