1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. TRP Channel
  3. TRPC4/5-IN-2

TRPC4/5-IN-2 (化合物 12) 是一种口服有效的瞬时受体电位 (TRPC5) 抑制剂,IC50 值为 81 nM。TRPC4/5-IN-2 具有良好的生物安全性和较低的肝肾毒性,有望在慢性肾脏疾病 (CKD) 治疗领域发挥重要作用。

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TRPC4/5-IN-2 Chemical Structure

TRPC4/5-IN-2 Chemical Structure

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Customer Review

查看 TRP Channel 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TRPC4/5-IN-2 (Compound 12) is an orally effective transient receptor potential (TRPC5) inhibitor with a IC50 value of 81 nM. TRPC4/5-IN-2 has good biosafety and low liver and kidney toxicity, and is expected to play an important role in the treatment of chronic kidney disease (CKD)[1].

IC50 & Target

TRPC5

 

体外研究
(In Vitro)

TRPC4/5-IN-2 (化合物 12) (30 μM, 24 h) 对肝细胞和 HK-2 肾细胞具有较低的细胞毒性[1]

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

Cell Viability Assay[1].

Cell Line: Hepatocyte, HK-2 cell
Concentration: 3, 10, 30 μM
Incubation Time: 24 h
Result: Didn’t affect cell growth on both primary cultured hepatocytes and HK-2 cells
体内研究
(In Vivo)

TRPC4/5-IN-2 (化合物 12) (10 mL/kg, p.o.,) 在雄性 ICR 小鼠中药代动力学情况良好,且低血脑屏障通过率避免了中枢神经系统中 TRPC5 活性的不必要抑制[1]
TRPC4/5-IN-2 (化合物 12) (500 mg/kg, p.o.,) 在 C57 小鼠中具有良好的生物安全性[1]
TRPC4/5-IN-2 (化合物 12) (10 mg/kg, p.o., 每天 2 次,持续 3 周) 对大鼠低血压性肾损伤具有疗效[1]

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

Animal Model: male ICR mice[1].
Dosage: 10 mL/kg
Administration: oral gavage (p.o.)
Result: Was well and rapidly absorbed and mainly distributed in the colon, kidney, and liver[1].
Animal Model: hypertensive renal injury rat model[1].
Dosage: 5, 10 mg/kg
Administration: oral gavage (p.o.)
Result: Suppressed levels of urinary protein and urinary albumin to creatinine ratio (UACR) and attenuated the degree of podocyte injury [1].
Animal Model: C57 mice[1].
Dosage: 10 mL/kg, the final dose is 500 mg/kg
Administration: oral gavage (p.o.)
Result: Didn't cause death or abnormal behavior in mice[1].
分子量

424.26

Formula

C18H16Cl2FN5O2

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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.

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产品名称:
TRPC4/5-IN-2
目录号:
HY-162584
需求量: