2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. PDE4-IN-30

PDE4-IN-30 是一种选择性的 PDE4 抑制剂，其对 PED4D2 的 IC50 为 2.7 nM，通过卤素键和金属配位作用靶向 PDE4。PDE4-IN-30 对其他 PDE 亚家族的选择性至少高出 67 倍。PDE4-IN-30 可用于特发性肺纤维化的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PDE4-IN-30

PDE4-IN-30 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

PDE4-IN-30 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

PDE4-IN-30 is a selective PDE4 inhibitor with an IC50 of 2.7 nM for PED4D2, targeting PDE4 through halogen bonding and metal coordination. PDE4-IN-30 exhibits at least 67-fold selectivity for other PDE subfamilies. PDE4-IN-30 can be used for the research of idiopathic pulmonary fibrosis[1].

IC50 & Target[1]

PDE4D2

2.7 nM (IC50)

PDE10A

181.8 nM (IC50)

PDE8A

1156 nM (IC50)

PDE5A

7491 nM (IC50)

体外研究
(In Vitro)

PDE4-IN-30 (compound 13c) (5 μM-20 μM；48 小时) 在 MRC-5 和 A549 细胞中有效抑制 TGF-β1 诱导的成纤维细胞向肌成纤维细胞转化 (FMT) 和上皮-间质转化 (EMT)[1]。
PDE4-IN-30 (5-20 μM；48 小时) 显著抑制 TGF-β1 诱导的 A549 细胞增殖和迁移[1]。
PDE4-IN-30 在 Caco-2 细胞中表现出良好的细胞渗透性和良好的药物样特性[1]。

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

PDE4-IN-30 相关抗体:

Western Blot Analysis[1]

Cell Line: MRC-5 and A549 cell lines
Concentration: 5 μM, 10 μM, 20 μM
Incubation Time: 48 h
Result: Significantly inhibited the overexpression of α-smooth muscle actin (α-SMA), COL1A1, and FN markers.
Downregulatedthe expression of N-cadherin and vimentin while it restored E-cadherin. expression to baseline levels.

Cell Proliferation Assay[1]

Cell Line: A549 cell lines
Concentration: 5 μM, 10 μM, 20 μM
Incubation Time: 48 h
Result: Significantly attenuated TGF-β1-induced A549 cell proliferation and migration.
体内研究
(In Vivo)

PDE4-IN-30 (compound 13c) (2.5 mg/kg，腹腔注射；治疗 3 周) 可改善 Bleomycin (BLM) (HY-17565A) 诱导的 C57BL/6J (6-8 周龄) 小鼠肺纤维化[1]。

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

Animal Model: Male C57BL/6J (6-8 weeks old; 18-22 g) were induced by a single intratracheal instillation of BLM (3 mg/kg)[1]
Dosage: 2.5 mg/kg
Administration: Intraperitoneal injection; 3 weeks of treatment starting from the second day post-BLM induction
Result: Significantly reduced lung coefficient, hydroxyproline levels, and fibrotic markers (FN1, COL1A1, α-SMA, N-cadherin, vimentin) while increasing E-cadherin expression.
Improved lung function parameters (inspiratory capacity (IC), forced vital capacity (FVC), lung compliance (Cchord), vital capacity (VC), peakexpiratory flow (PEF)) and reduced airway resistance.
Histological analysis showed reduced alveolar fibrosis and inflammatory infiltration. 
分子量

409.24

Formula

C14H17BrN8O2
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

PDE4-IN-30 相关分类

  • 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.

Keywords:

PDE4-IN-30Phosphodiesterase (PDE)PDE4 inhibitorantifibrotic activitypotency enhancementhigh affinitypyrazolo[1,5-]pyrimidinehalogen-bindinghepatic microsomal stabilitypulmonary fibrosisPDE4metal-coordinationInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
PDE4-IN-30
目录号：
HY-179639
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z