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

Iptacopan (LNP023) TFA 是一种有效的，具有口服活性的高选择性的 factor B 抑制剂，IC50 值为 10 nM，KD 为 7.9 nM。Iptacopan TFA 通过在补体级联反应中发挥近端作用，防止 PNH 中红细胞的破坏 (溶血) 以及 IgAN 和 C3G 中肾细胞的损伤。Iptacopan TFA 可用于研究补体介导疾病，特别是阵发性睡眠性血红蛋白尿症 (PNH)、原发性免疫球蛋白 A 肾病 (IgAN) 和补体 3 肾小球病 (C3G)。

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CAS No. : 1644670-38-1

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Iptacopan TFA 相关抗体

Top Publications Citing Use of Products

    Iptacopan TFA purchased from MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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.

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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].

    体外研究
    (In Vitro)

    Iptacopan (LNP023) TFA 在 50% 人血清中表现出对旁路补体途径 (AP) 诱导的膜攻击复合物 (MAC) 形成的强效抑制作用 (IC50 值为 130 nM)[2]。
    Iptacopan (LNP023) TFA 相对于其他蛋白酶表现出优异的选择性，在 41 种人类蛋白酶（包括 AP 蛋白因子 D (>100 μM)）中，其 IC50 值为 >30 μM[3]。

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

    Iptacopan TFA 相关抗体:
    体内研究
    (In Vivo)

    Iptacopan (LNP023；20-180 mg/kg；口服) TFA 可预防小鼠 KRN (150 μL) 诱发的关节炎，并且在大鼠膜性肾病实验模型中，预防性和治疗性给药均有效[2]。
    LNP023 TFA 口服给药 (大鼠 30 和狗 10 mg/kg) 后表现出中等半衰期 (T1/2；Wistar Han 大鼠 3.4 小时，比格犬 5.5 小时) 和 Cmax (Wistar Han 大鼠 410 nM，比格犬 2200 nM) [3]。
    Iptacopan TFA 静脉给药 (大鼠 1.0 和狗 0.1 mg/kg) 后表现出终末消除半衰期 (T1/2；Wistar Han 大鼠 7 小时，比格犬 5.6 小时)[3]。

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

    536.55

    Formula

    C27H31F3N2O6
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    Iptacopan TFA 相关分类

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    • 稀释计算器

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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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    目录号：
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