2. Metabolic Enzyme/Protease Apoptosis
  3. Phosphodiesterase (PDE) TNF Receptor
  4. PDE4-IN-34

PDE4-IN-34 是一种磷酸二酯酶 4 (PDE4) 抑制剂，对 PDE4B1、PDE4D2 的 IC50 值分别为 19 和 14 pM。PDE4-IN-34 对 PDE8A1 表现出微弱的抑制活性，IC50 值为 4.092 μM，对其他亚型有显著的选择性 (IC50 > 10 μM)。PDE4-IN-34 可在香烟烟雾联合 LPS (HY-D1056) 诱导的大鼠模型中改善肺功能、减少炎症反应并减轻肺组织损伤。PDE4-IN-34 可用于慢性阻塞性肺疾病的相关研究。

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PDE4-IN-34

PDE4-IN-34 Chemical Structure

CAS No. : 3052591-16-6

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PDE4-IN-34 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 TNF Receptor 亚型特异性产品:

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PDE4-IN-34 is a phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 19 pM and 14 pM against PDE4B1 and PDE4D2, respectively. PDE4-IN-34 shows weak inhibitory activity against PDE8A1, with an IC50 value of 4.092 μM, and exhibits significant selectivity over other subtypes (IC50 > 10 μM). PDE4-IN-34 improves pulmonary function, reduces inflammatory responses and alleviates lung tissue damage in a rat model induced by cigarette smoke combined with LPS (HY-D1056). PDE4-IN-34 can be used for research related to chronic obstructive pulmonary disease[1].

IC50 & Target[1]

PDE4B1

19 pM (IC50)

PDE4D2

14 pM (IC50)

PDE8A1

4.092 μM (IC50)

体外研究
(In Vitro)

PDE4-IN-34 (Compound P29) (1 fM-1 µM; 18 h) 可强效抑制 LPS 诱导的人外周血单个核细胞 (PBMCs) 中 TNF-α 的释放，其 IC50 为 0.3 nM[1]。
PDE4-IN-34 (1 μM; 6 h) 在 1 μM 浓度下可与 99.5%的人血浆蛋白结合[1]。
PDE4-IN-34 (1 μM) 可在人肝微粒体中代谢，肝清除率为 0.0522 mL/min/mg，半衰期为 26.6 min[1]。
PDE4-IN-34 在最高 30 μM 的浓度下不会显著抑制 hERG 钾离子通道，提示心脏毒性风险较低[1]。
PDE4-IN-34 在最高 10 μM 的浓度下不会显著抑制人肝脏 CYP1A2、CYP2C9、CYP2C19、CYP2D6 或 CYP3A4 酶，提示药物间相互作用风险较低[1]。

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

PDE4-IN-34 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax T1/2 AUC0-t AUC0-∞ MRT0-t MRT0-∞ Bioavailability Vz CL
Rat[1] 3 mg/kg i.v. 754 ng/mL 0.083 h 4.46 h 4458 ng·h/mL 4919 ng·h/mL 4.80 h 6.39 h / 4317 mL/kg 681 mL/h/kg
Rat[1] 10 mg/kg p.o. 92.0 ng/mL 1.5 h 10.3 h 1225 ng·h/mL 1637 ng·h/mL 8.45 h 14.7 h 9.99 % / /
体内研究
(In Vivo)

PDE4-IN-34 (Compound P29) (0.1-3 μmol/kg; 气管给药; 每日一次共 28 天) 可通过抑制炎症细胞活性和细胞因子释放，呈剂量依赖性缓解香烟烟雾和 LPS 诱导的大鼠 COPD[1]。
PDE4-IN-34 (3-10 mg/kg; 气管给药; 单次给药) 对比格犬的吸入剂量高达 10 mg/kg 时不会引发呕吐[1]。

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

Animal Model: Sprague-Dawley (SD) (male, 200-250 g, COPD induced by intratracheal LPS instillation on days 1 and 14 plus daily cigarette smoke exposure from days 2 to 28)[1]
Dosage: 0.1 μmol/kg; 1 μmol/kg; 3 μmol/kg
Administration: intratracheal inhalation; once daily; 28 days
Result: Produced a dose-dependent reduction in white blood cell counts, eosinophils, neutrophils, and lymphocytes in BALF.
Caused a dose-dependent reduction in inflammatory markers including IL-1β, TNF-α, and IL-6 in serum, lung tissue, and BALF, with significant effects observed at 1 μmol/kg and maximal effects at 3 μmol/kg.
Led to notable improvements in lung structure at 3 μmol/kg dose, with reduced alveolar wall disruption, interstitial thickening, and inflammatory cell infiltration compared to the vehicle-treated group.
Showed significantly reduced inflammatory cell infiltration at 0.1 and 1 μmol/kg doses relative to the vehicle group.
分子量

381.64

Formula

C17H11Cl3N2O2
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

PDE4-IN-34 相关分类

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  • 稀释计算器

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  • 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-343052591-16-6Phosphodiesterase (PDE)TNF ReceptorTumor Necrosis Factor ReceptorTNFRPDE4D2 enzymephosphodiesterase 4rat modelschronic obstructive pulmonary diseaseperipheral blood mononuclear cellshuman PBMCsPDE4B1 enzymePDE4human PDE4human liver microsomesInhibitorinhibitorinhibit

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