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

Iptacopan (LNP023) is an effective and orally-active highly selective factor B inhibitor with an IC50 value of 10 nM and KD of 7.9 nM. Iptacopan exerts a proximal effect in the complement cascade reaction, preventing the destruction (hemolysis) of red blood cells in PNH and the damage of renal cells in IgAN and C3G. Iptacopan can be used for the study of complement-mediated diseases, particularly paroxysmal nocturnal hemoglobinuria (PNH), primary immunoglobulin A nephropathy (IgAN), and complement 3 glomerulopathy (C3G).

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

CAS No. : 1644670-37-0

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

Based on 13 publication(s) in Google Scholar

Other Forms of Iptacopan:

Iptacopan Related Antibodies

Top Publications Citing Use of Products

    Iptacopan purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec;17(1):2484386.  [Abstract]

    Western blot analysis of HIF-1α protein expression in M28-trained macrophages 3 days after inhibition of CFB (Iptacopan, 10 µM) or C3aR (SB290157, 10 µM). Data were presented as means ± SEM.

    Iptacopan purchased from MedChemExpress. Usage Cited in: Gut Microbes. 2025 Dec;17(1):2484386.  [Abstract]

    After pretreatment with the Iptacopan (CFB inhibitor) and SB290157 (C3aR inhibitor, 10 µM) for 24 hours, cells were treated with M28 (5 µg/mL) for an additional 24 hours. The cells were then washed twice with PBS to remove M28, and incubation was continued. 5 days later, macrophages were lysed to assess the phosphatidylcholine content. The results showed that, following treatment with the inhibitor, the phosphatidylcholine content within M28-trained macrophages decreased.

    Iptacopan purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2023 Oct 5;30(10):1315-1330.e10.  [Abstract]

    Relative quantification of blood perfusion area in human vessels after Iptacopan (LNP023, 25 mg/kg; p.o.; 1 h before extracellular domain (ECD) injection) and spike-ECD or sham (ECD+DMSO) treatment to before treatment (mean ± SE; n = 3; Welch’s t-test; **p < 0.01). The results showed that LNP023 effectively inhibited thrombus formation in an engineered human vascular model.

    Iptacopan purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2023 Oct 5;30(10):1315-1330.e10.  [Abstract]

    Intravital imaging of the organoid-transplanted mice treated with complement factor B inhibitor LNP023 and spike-ECD. Iptacopan (LNP023, 25 mg/kg; p.o) was orally administrated 1 hr before spike-ECD treatment. The organoid-derived human vascular and blood flow are visualized using a hCD31 and FITC-dextran, respectively.

    Iptacopan purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2022 Sep:153:113433.

    Iptacopan (LNP023, 30 mg/kg; gavage; once daily for 2 weeks) alleviated skin lesions, alopecia, and splenomegaly, effectively improving the lupus-like signs in MRL/lpr mice.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Iptacopan (LNP023) is an effective and orally-active highly selective factor B inhibitor with an IC50 value of 10 nM and KD of 7.9 nM. Iptacopan exerts a proximal effect in the complement cascade reaction, preventing the destruction (hemolysis) of red blood cells in PNH and the damage of renal cells in IgAN and C3G. Iptacopan can be used for the study of complement-mediated diseases, particularly paroxysmal nocturnal hemoglobinuria (PNH), primary immunoglobulin A nephropathy (IgAN), and complement 3 glomerulopathy (C3G)[1][2][3].

    IC50 & Target

    KD: 7.9 nM (factor B)[2]
    IC50: 10 nM (factor B)[2]
    In Vitro

    Iptacopan (LNP023) demonstrates potent inhibition of alternative complement pathway (AP)-induced membrane attack complex (MAC) formation in 50% human serum (IC50 value of 130 nM)[2].
    Iptacopan (LNP023) exhibits excellent selectivity over other proteases affording IC50 values of >30 μM across a panel of 41 human proteases, including the AP protein factor D (>100 μM)[3].

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

    Iptacopan Related Antibodies
    In Vivo

    Iptacopan (LNP023; 20-180 mg/kg; oral administration) prevents KRN (150 μL)-induced arthritis in mice and is effective upon prophylactic and therapeutic dosing in an experimental model of membranous nephropathy in rats[2].
    LNP023 exhibits moderate half-lives (T1/2; Wistar Han rats 3.4 h, beagle dogs 5.5 h) and Cmax (Wistar Han rats 410 nM, beagle dogs 2200 nM) following oral administration (rat 30 and, dog 10 mg/kg)[3].
    Iptacopan exhibits terminal elimination half-lives (T1/2; Wistar Han rats 7 h, beagle dogs 5.6 h) due to high plasma clearance (8, and 2 mL/min/kg respectively combined with large volumes of distribution (2.3, and 0.6 L/kg respectively) following intravenous administration (rat 1.0 and, dog 0.1 mg/kg)[3].

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

    Animal Model: C57BL/6 mice with KRN-induced arthritis[2]
    Dosage: 20, 60, and 180 mg/kg
    Administration: Orally gavaged; twice a day (b.i.d.) for 14 days
    Result: Blocked KRN-induced arthritis.
    Clinical Trial
    Molecular Weight

    422.52

    Formula

    C25H30N2O4
    CAS No.
    Appearance

    Solid

    Color

    Gray to brown

    SMILES

    O=C(O)C1=CC=C([C@H]2N(CC3=C(OC)C=C(C)C4=C3C=CN4)CC[C@H](OCC)C2)C=C1
    Shipping

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

    DMSO : 50 mg/mL (118.34 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 2.3668 mL 11.8338 mL 23.6675 mL
    5 mM 0.4734 mL 2.3668 mL 4.7335 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • 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: ≥ 5 mg/mL (11.83 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5 mg/mL (11.83 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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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 +
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    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: 99.95%

    SDS (393 KB)

    COA (252 KB) HNMR (750 KB) RP-HPLC (253 KB) LCMS (93 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3668 mL 11.8338 mL 23.6675 mL 59.1688 mL
    5 mM 0.4734 mL 2.3668 mL 4.7335 mL 11.8338 mL
    10 mM 0.2367 mL 1.1834 mL 2.3668 mL 5.9169 mL
    15 mM 0.1578 mL 0.7889 mL 1.5778 mL 3.9446 mL
    20 mM 0.1183 mL 0.5917 mL 1.1834 mL 2.9584 mL
    25 mM 0.0947 mL 0.4734 mL 0.9467 mL 2.3668 mL
    30 mM 0.0789 mL 0.3945 mL 0.7889 mL 1.9723 mL
    40 mM 0.0592 mL 0.2958 mL 0.5917 mL 1.4792 mL
    50 mM 0.0473 mL 0.2367 mL 0.4734 mL 1.1834 mL
    60 mM 0.0394 mL 0.1972 mL 0.3945 mL 0.9861 mL
    80 mM 0.0296 mL 0.1479 mL 0.2958 mL 0.7396 mL
    100 mM 0.0237 mL 0.1183 mL 0.2367 mL 0.5917 mL
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    Iptacopan 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:

    Iptacopan1644670-37-0LNP023LNP 023LNP-023Complement Systemfactor BalternativepathwayAPcomplementsystempathogenesisparoxysmalnocturnalhemoglobinuriaPNHatypicalhemolyticuremicsyndromeunderlyingcausecomplement 3glomerulopathyC3GInhibitorinhibitorinhibit

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