TRPC6-IN-1

• 常用名: TRPC6-IN-1
• 英文名: TRPC6-IN-1
• CAS号: 901715-05-7
• 分子量: 398.43
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₁H₂₃FN₄O₃
• 熔点: N/A
• 闪点: N/A

TRPC6-IN-1用途

TRPC6-IN-1 是 TRPC6 的一个抑制剂,其 EC50 值为 4.66 μM。

TRPC6-IN-1名称

• 中文名: TRPC6-IN-1
• 英文名: TRPC6-IN-1

TRPC6-IN-1生物活性

• 描述: TRPC6-IN-1 是 TRPC6 的一个抑制剂,其 EC50 值为 4.66 μM。
• 相关类别:
  信号通路 >> 跨膜转运 >> TRP频道
  研究领域 >> 其他
• 靶点实验:

  EC50: 0.45 μM (TRPC3), 1.13 μM (TRPC7), 4.66 μM(TRPC3)[1].

• 体外研究: TRPC6-IN-1(化合物4o)以浓度依赖性方式在TRPC6细胞中上升,平均EC50值为4.66±0.03μM,证明化合物对TRPC6的活性与原始铅相当。还在共表达μ阿片受体(MOR)和TRPC4β的HEK293细胞上测试TRPC6-IN-1,其与TRPC3/6/7属于TRPC通道的不同亚组。在μ激动剂刺激后,这些细胞显示出[Ca 2+] i的强烈增加。 TRPC6-IN-1还在表达人TRPC3的HEK293细胞中唤起全细胞电流。 TRPC6-IN-1引发TRPC7细胞中浓度依赖性电流增加。与TRPC6不同,即使使用低Ca2 +(0.1mM)浴溶液,电流在负电位和正电位的高TRPC6-IN-1浓度(10和30μM)中也显示出一些脱敏。尽管如此,仍然在<10μMTRPC6-IN-1 [1]检测到TRPC7电流的逐步增加。
• 参考文献:

  [1]. Qu C, et al. Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels. J Med Chem. 2017 Jun 8;60(11):4680-4692.

TRPC6-IN-1物理化学性质

• 分子式: C₂₁H₂₃FN₄O₃
• 分子量: 398.43
• InChIKey: OXPMSNBGJOEGSC-UHFFFAOYSA-N
• SMILES: CCOC(=O)N1CCC(c2cc(=O)n3[nH]c(C)c(-c4ccc(F)cc4)c3n2)CC1
• 外观性状: 固体
• 储存条件: 2-8°C，密封，干燥

TRPC6-IN-1靶点实验

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