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AC1903

AC1903是一种选择性的TRPC5抑制剂，具有足细胞保护特性，对 TRPC4 或 TRPC6没有影响，并且在激酶谱分析中没有显示出脱靶效应。在局灶节段性肾小球硬化大鼠模型中，AC1903抑制严重蛋白尿，并且防止足细胞丢失。

CAS号

831234-13-0

分子式

C19H17N3O

主要靶点

TRP/TRPV Channel

仅限科研使用

Cat No : CM06817

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Synonyms

验证数据展示

  • CAS No.: 831234-13-0

    AC1903
    CAS#: 831234-13-0

产品信息

AC1903 is a specific inhibitor of TRPC5 channel, and has been shown to suppress severe proteinuria and prevent podocyte loss.

CAS号 831234-13-0
分子式 C19H17N3O
主要靶点 TRP/TRPV Channel
主要通路 离子通道
分子量 303.36
纯度 98.33%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

TRPC5 current IN HEK-293 cells:14.7 μM (IC50)

体内活性

AC1903, that specifically blocks TRPC5 channel activity in glomeruli of proteinuric rats.?Chronic administration of AC1903 suppressed severe proteinuria and prevented podocyte loss in a transgenic rat model of FSGS.AC1903 also provided therapeutic benefit in a rat model of hypertensive proteinuric kidney disease.?TRPC5 activity drives disease and that TRPC5 inhibitors may be valuable for the treatment of progressive kidney diseases[1].

溶解度

DMSO:32.5 mg/mL (107.13 mM)

动物实验

Twice-daily intraperitoneal injections of AC1903 (50 mg/kg) for 7 days suppressed severe proteinuria in AT1R Tg rats (Advanced)[1]

参考文献

1.Yiming Zhou, et al. A small-molecule inhibitor of TRPC5 ion channels suppresses progressive kidney disease in animal models. Science
2.Sharma S H , Pablo J L , Montesinos M S , et al. Design, synthesis and characterization of novel N-heterocyclic-1-benzyl-1H-benzo[d]imidazole-2-amines as selective TRPC5 inhibitors leading to the identification of the selective compound, AC1903[J]. Bioorganic & Medicinal Chemistry Letters, 2018.

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