1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. PDE1-IN-10

PDE1-IN-10 是一种强效且选择性的 磷酸二酯酶 1 (PDE1) 抑制剂,其 IC50 为 5 nM。PDE1-IN-10 能够抑制 TGF-β/Smad-MAPK 信号通路,并具有抗纤维化作用。PDE1-IN-10 可用于特发性肺纤维化的研究。

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PDE1-IN-10

PDE1-IN-10 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PDE1-IN-10 is a potent and sekective Phosphodiesterase 1 (PDE1) inhibitor with an IC50 of 5 nM. PDE1-IN-10 can suppress TGF-β/Smad-MAPK signaling and exhibit antifibrotic effects. PDE1-IN-10 can be used for the research of idiopathic pulmonary fibrosis[1].

IC50 & Target[1]

PDE1

5 nM (IC50)

体外研究
(In Vitro)

PDE1-IN-10 (Compound 4b) (1-5 μM, 48 h) 可降低 TGF-β1 诱导的 MRC-5 细胞中 α-平滑肌肌动蛋白、I 型胶原蛋白和纤连蛋白的水平[1]
PDE1-IN-10 (1-5 μM, 48 h) 可抑制 MRC-5 细胞中的 TGF-β/Smad-MAPK 信号通路[1]

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

Western Blot Analysis[1]

Cell Line: TGF-β1-induced MRC-5 cells
Concentration: 1, 2.5 and 5 μM
Incubation Time: 48 h
Result: Reduced α-SMA, collagen I and fibronectin levels.
Reduced p-p38, p-ERK1/2, p-Smad2, and p-Smad3 levels.
Increased PKA, PKG and p-CREB levels.
体内研究
(In Vivo)

PDE1-IN-10 (Compound 4b) (2.5 mg/kg,腹腔注射,每日一次,持续 4 周) 在 Bleomycin (HY-108345) 诱导的 SD 大鼠肺纤维化模型中表现出抗纤维化作用[1]

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

Animal Model: Bleomycin (HY-108345)-induced pulmonary fibrosis models of SD rats[1]
Dosage: 2.5 mg/kg
Administration: Intraperitoneally injection, daily for 4 weeks
Result: Alleviated alveolar inflammation and collagen deposition.
Inhibited the overexpression of α-SMA in lung tissues.
Downregulated α-SMA, vimentin and collagen I, upregulates E-cadherin.
分子量

423.41

Formula

C24H19F2NO4

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:
PDE1-IN-10
目录号:
HY-175971
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