2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. PDE1-IN-7

PDE1-IN-7 (Compound 13h) 是 bPDE1 的选择性抑制剂 (IC50=10 nM)。在 BDL 诱导的肝纤维化大鼠模型中表现出显著的抗纤维化效果。PDE1-IN-7 可以用于肝纤维化方面的研究。

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PDE1-IN-7

PDE1-IN-7 Chemical Structure

CAS No. : 3027833-49-1

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PDE1-IN-7 相关抗体

Top Publications Citing Use of Products

查看 Phosphodiesterase (PDE) 亚型特异性产品:

查看所有亚型
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PDE1-IN-7 (Compound 13h) is a selective inhibitor of bPDE1 (IC50= 10 nM). PDE1-IN-7 exhibits significant anti-fibrotic effects in a BDL-induced liver fibrosis rat model. PDE1-IN-7 can be used for research in liver fibrosis[1].

IC50 & Target[1]

PDEI

10 nM (IC50)

体外研究
(In Vitro)

PDE1-IN-7 (2.5-20μM; 48 h) 能够有效抑制 TGF-β 诱导的 LX-2 细胞成肌纤维细胞分化和增殖[1]。

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

PDE1-IN-7 相关抗体:

Western Blot Analysis[1]

Cell Line: human stellate cell LX-2
Concentration: 2.5, 5, 10, 20 μM
Incubation Time: 48 h
Result: Dose-dependently reduced the elevated expression levels of fibronectin, collagen I, and α-SMA induced by TGF-β in LX-2 cells.
体内研究
(In Vivo)

PDE1-IN-7 (i.p.; 2.5 mg/kg; 每天一次，持续 21 天) 在胆管结扎 (BDL) 诱导的肝纤维化大鼠模型中表现出显著的抗纤维化效果[1]。


药代动力学分析[1]

Route Dose (mg/kg) t1/2 (h) Cmax (ng/mL) AUC∞ (h)(ng·/mL) Clobs (mL/min/kg) MRT (h) Vss_obs (mL/kg)
i.v. 2.5 7.51 ± 0.64 25,006 ± 3082 6317 ± 839 6.56 ± 0.81 1.77 ± 0.07 698 ± 104

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

Animal Model: BDL-induced hepatic fibrosis rats[1]
Dosage: 2.5 mg/kg
Administration: i.p.; once daily for 21 days
Result: Significantly reduced alanine transaminase (ALT), aspartate transaminase (AST) and total bile acids (TBA) levels.
Reduced structural damage to liver tissue, decreased fibrotic foci, and lowered collagen deposition levels.
Significantly reduced protein expression levels at α-SMA and collagen I levels.
Significantly increased cAMP levels.
分子量

614.70

Formula

C32H36F2N2O6S
CAS 号
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

PDE1-IN-7 相关分类

  • 摩尔计算器

  • 稀释计算器

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

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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.

Keywords:

PDE1-IN-73027833-49-1Phosphodiesterase (PDE)antifibroticCAMP level regulationBDL-induced hepatic fibrosisInhibitorinhibitorinhibit

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