2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. Phosphodiesterase (PDE) Interleukin Related
  4. PDE3/4-IN-4

PDE3/4-IN-4 是一种口服有效的 PDE3A 和 PDE4B 抑制剂，其对 PDE3A 的 IC50 为 10 nM，对 PDE4B 的 IC₅₀ 为 9.4 nM，且相对于大多数其他 PDE 家族成员表现出选择性活性。PDE3/4-IN-4 可调控 cAMP/PKA/CREB 信号通路。PDE3/4-IN-4 可抑制促炎因子 IL-6。PDE3/4-IN-4 可降低肝组织中炎性标志物的表达。PDE3/4-IN-4 可减轻肝纤维化程度。PDE3/4-IN-4 可限制胆汁淤积和脓毒症诱导的肝病小鼠模型中的肝损伤。PDE3/4-IN-4 可用于肝损伤、胆汁淤积性肝病、脓毒症诱导的肝损伤相关研究 。

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PDE3/4-IN-4

PDE3/4-IN-4 Chemical Structure

CAS No. : 3088024-27-2

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PDE3/4-IN-4 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

查看 Interleukin Related 亚型特异性产品:

查看所有亚型
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PDE3/4-IN-4 is an orally active PDE3A and PDE4B inhibitor with IC50 values of 10 nM and 9.4 nM, respectively. PDE3/4-IN-4 shows selective activity relative to most other PDE family members. PDE3/4-IN-4 modulates the cAMP/PKA/CREB signaling pathway. PDE3/4-IN-4 inhibits pro-inflammatory factor IL-6. PDE3/4-IN-4 reduces expression of inflammatory markers in liver tissue. PDE3/4-IN-4 attenuates liver fibrosis. PDE3/4-IN-4 limits liver damage in cholestatic and sepsis-induced liver disease mice models. PDE3/4-IN-4 can be used for the research of liver injury, cholestatic liver diseases, sepsis-induced liver injury[1].

IC50 & Target[1]

PDE3A

10 nM (IC50)

PDE4B

9.4 nM (IC50)

PDE10A

477.9 nM (IC50)

PDE6C

5739 nM (IC50)

PDE1A

>10000 nM (IC50)

PDE2A

>10000 nM (IC50)

PDE5A

>10000 nM (IC50)

PDE7A

>10000 nM (IC50)

PDE8A

>10000 nM (IC50)

PDE11A

>10000 nM (IC50)

IL-6

 

体外研究
(In Vitro)

PDE3/4-IN-4 (compound D5) (10-60 μM；作用 24 h) 在浓度高达 60 μM、作用 24 h 的条件下，对人正常肝细胞 LO2 未表现出显著毒性[1]。
PDE3/4-IN-4 (compound D5) 可抑制 Lipopolysaccharides (LPS) (HY-D1056) 刺激的 LO2 细胞中 IL-6 的分泌，其 IC50 为 14.89 μM[1]。
PDE3/4-IN-4 (compound D5)(15 μM；LPS 刺激前预处理 12 h) 可上调 LPS 诱导的 LO2 细胞中 p-CREB 和 p-PKA 的表达[1]。
PDE3/4-IN-4 (compound D5) 在小鼠、大鼠、犬、猴及人肝微粒体中具有充足的代谢稳定性[1]。

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

PDE3/4-IN-4 相关抗体:

Western Blot Analysis[1]

Cell Line: LPS-induced LO2 cells
Concentration: 15 μM (pre-treatment before LPS stimulation)
Incubation Time: 12 h (pre-treatment before 4 h LPS stimulation)
Result: Markedly increased the expression of phosphorylated CREB (p-CREB) and phosphorylated PKA (p-PKA) compared to LPS-induced cells; confirmed increased p-CREB expression via immunofluorescence staining.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-t AUC0-∞ Cmax T1/2 Tmax F C0 Vz CL
Mice[1] 5 mg/kg i.v. 13909.7 ng·h/mL 13931.6 ng·h/mL / 2.134 h / / 18302.0 ng/mL 1122.9 mL/kg 370.0 mL/h/kg
Mice[1] 10 mg/kg p.o. 3479.9 ng·h/mL 3489.3 ng·h/mL 922.4 ng/mL 1.4 h 1.0 h 12.5 % / / /
体内研究
(In Vivo)

PDE3/4-IN-4 (compound D5) (10-40 mg/kg；灌胃；每日一次；连续 7 天) 可减轻胆管结扎术 (BDL) 小鼠的肝脏炎症与纤维化，其中 40 mg/kg 剂量的疗效更优[1]。
PDE3/4-IN-4 (10-40 mg/kg；灌胃；每日一次；连续 7 天) 可减轻盲肠结扎穿刺术 (CLP) 小鼠的肝脏炎症与损伤，其中 40 mg/kg 剂量的效果更显著[1]。

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

Animal Model: C57BL/6 (male, 18-22 g, bile duct ligation surgery)[1]
Dosage: 10 mg/kg; 40 mg/kg
Administration: p.o.; daily; 7 days
Result: Significantly reduced hepatic mRNA expression of IL-6 and IL-1β; reduced total bile acid (TBA) and alanine aminotransferase (ALT) levels; partially restored liver architecture (HE staining); increased hepatic p-CREB and p-PKA expression; reduced collagen deposition (Masson staining, 40 mg/kg only); showed greater efficacy at 40 mg/kg.
Animal Model: C57BL/6 (male, 18-22 g, cecal ligation and puncture surgery)[1]
Dosage: 10 mg/kg; 40 mg/kg
Administration: p.o.; daily; 7 days
Result: Reduced hepatic mRNA expression of IL-6 and IL-1β; reduced total bile acid (TBA), aspartate aminotransferase (AST), and alanine aminotransferase (ALT) levels; increased hepatic p-CREB and p-PKA expression; reduced hepatic inflammatory cell infiltration and restored hepatocyte structure (HE staining, 40 mg/kg only); reduced collagen deposition (Masson staining, 40 mg/kg only); showed greater efficacy at 40 mg/kg.
分子量

559.56

Formula

C30H27F2N5O4
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

PDE3/4-IN-4 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

PDE3/4-IN-43088024-27-2Phosphodiesterase (PDE)Interleukin RelatedILliver tissueIL-6cholestatic liver diseasesliver microsomescAMP/PKA/CREB signaling pathwayLO2 human normal liver cellsPDE3Asepsis-induced liver injuryPDE4Bliver fibrosisInhibitorinhibitorinhibit

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