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AC1903

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

HEK-293|inhibit|FSGS|glomerulosclerosis|focal segmental|AC 1903|AC1903|AC-1903|kidney disease|Inhibitor|proteinuria|podocyte loss|ros|TRP Channel|TRPC5|Transient receptor potential channels|TRPChannel|TRPV Channel|TRPVChannel

验证数据展示

  • CAS No.: 831234-13-0

    AC1903
    CAS#: 831234-13-0

产品信息

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 98.45%， 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 | Shipping with blue ice.
别名 HEK-293|inhibit|FSGS|glomerulosclerosis|focal segmental|AC 1903|AC1903|AC-1903|kidney disease|Inhibitor|proteinuria|podocyte loss|ros|TRP Channel|TRPC5|Transient receptor potential channels|TRPChannel|TRPV Channel|TRPVChannel

靶点活性

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

体内活性

AC1903是一种特异性阻断蛋白尿大鼠肾小球TRPC5通道活动的化学化合物。通过持续给药，AC1903能有效抑制严重的蛋白尿，并在FSGS转基因大鼠模型中防止足细胞丧失。此外，AC1903还在高血压性蛋白尿肾病大鼠模型中提供了治疗效益。TRPC5的活动推动了疾病的进展，因此TRPC5抑制剂可能是治疗进展性肾病的有价值的化合物[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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