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

Iptacopan (LNP023) TFA 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 TFA 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 TFA 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).

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CAS No. : 1644670-38-1

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Iptacopan TFA Related Antibodies

Top Publications Citing Use of Products

    Iptacopan TFA 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 TFA 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 TFA 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 TFA 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 TFA 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.

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    Description

    Iptacopan (LNP023) TFA 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 TFA 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 TFA 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].

    In Vitro

    Iptacopan (LNP023) TFA 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) TFA 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 TFA Related Antibodies
    In Vivo

    Iptacopan (LNP023; 20-180 mg/kg; oral administration) TFA 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 TFA 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 TFA 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.
    Molecular Weight

    536.55

    Formula

    C27H31F3N2O6
    CAS No.
    SMILES

    C(C(O)=O)(F)(F)F.C(C1=C2C(=C(C)C=C1OC)NC=C2)N3[C@@H](C[C@@H](OCC)CC3)C4=CC=C(C(O)=O)C=C4
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    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
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    Iptacopan TFA Related Classifications

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    • 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:

    Iptacopan1644670-38-1LNP023LNP 023LNP-023Complement Systemfactor BalternativepathwayAPcomplementsystempathogenesisparoxysmalnocturnalhemoglobinuriaPNHatypicalhemolyticuremicsyndromeunderlyingcausecomplement 3glomerulopathyC3GInhibitorinhibitorinhibit

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