2. Metabolic Enzyme/Protease TGF-beta/Smad Stem Cell/Wnt Immunology/Inflammation Apoptosis Cytoskeleton
  3. Phosphodiesterase (PDE) PKA Interleukin Related TNF Receptor Collagen
  4. Phosphodiesterase-IN-5

Phosphodiesterase-IN-5 是一种强效、口服有效的选择性磷酸二酯酶 10A (PDE10A) 抑制剂，IC50 值为 6.2 nM。Phosphodiesterase-IN-5 对其他 PDE 亚型表现出 1612 倍以上的选择性。Phosphodiesterase-IN-5 通过阻断 cAMP/PKA/CREB ​​信号通路，抑制肌成纤维细胞分化，在 Bleomycin (BLM) (HY-108345) 诱导的小鼠肺纤维化 (PF) 模型中表现出显著的抗纤维化作用。Phosphodiesterase-IN-5 可用于肺纤维化的研究。

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Phosphodiesterase-IN-5

Phosphodiesterase-IN-5 Chemical Structure

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Phosphodiesterase-IN-5 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 PKA 亚型特异性产品:

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PKA PKAR PKACα

查看 Interleukin Related 亚型特异性产品:

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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

查看 TNF Receptor 亚型特异性产品:

查看所有亚型
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

Phosphodiesterase-IN-5 is a potent, orally active and selective phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 6.2 nM. Phosphodiesterase-IN-5 shows >1612-fold selectivity over other PDEs. Phosphodiesterase-IN-5 exhibits potent antifibrotic efficacy in a Bleomycin (BLM) (HY-108345)-induced murine model of pulmonary fibrosis (PF) by blocking myofibroblast differentiation via the cAMP/PKA/CREB signaling pathway. Phosphodiesterase-IN-5 can be used for the research of PF[1].

IC50 & Target[1]

PDE10A

6.2 nM (IC50)

体外研究
(In Vitro)

Phosphodiesterase-IN-5 (compound QC-3) (5-20 μM；48 小时) 通过激活 cAMP/PKA/CREB ​​通路，在 TGF-β1 (HY-163536) 刺激的 MRC-5 细胞中表现出抗纤维化活性，从而抑制肌成纤维细胞分化和 ECM 沉积[1]。
Phosphodiesterase-IN-5 与 PDE10A 的催化结构域结合，与 Gln726 形成氢键，与 Ile692 形成疏水相互作用，而 6-F 取代基能够通过水分子与 Asp674 形成卤键[1]。

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

Phosphodiesterase-IN-5 相关抗体:

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell [1]

Cell Line: MRC-5 cells
Concentration: 3.125, 6.25, 12.5, 25, 50, 100, 200 μM
Incubation Time: 48 h
Result: Showed no cytotoxic in MRC-5 cells at concentrations up to 200 μM.

Western Blot Analysis[1]

Cell Line: TGF-β1-stimulated MRC-5 cells
Concentration: 5, 10, 20 μM
Incubation Time: 48 h
Result: Demonstrated concentration-dependent reductions in FN, COL-I, and α-SMA protein expression.
体内研究
(In Vivo)

Phosphodiesterase-IN-5 (10 mg/kg，灌胃，每日一次，持续 21 天) 通过 cAMP/PKA/CREB ​​信号通路阻断肌成纤维细胞分化，在 BLM 诱导的小鼠 PF 模型中表现出强大的抗纤维化功效[1]。

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

Animal Model: Male C57BL/6 mice (7-9 weeks old, 20-24 g) induced by BLM[1]
Dosage: 2.5, 5, 10 mg/kg
Administration: i.g.; daily for 21 days
Result: Dose-dependently reversed BLM-induced changes in Penh, endexpiratory pause (EEP), relaxation time (RT), andfrequency (f), nearly restoring them to normal levels.
Mitigated BLM-induced body weight loss and elevated lung coefficient in a dose-dependent manner.
Reduced IL-6 and TGF-β levels in broncho alveolar lavage fluid (BALF), and restored pulmonary cAMP levels.
Markedly reduced BLM-induced increases in IL-6 and TGF-β levels in BALF, with the mos pronounced inhibition observed at the 10 mg/kg dose.
Restored pulmonary cAMP levels.
Improved pulmonary morphology.
Effectively reduced the level of alveolar wall thickening, inflammatory cell infiltration, and collagen deposition.
Showed a dose-dependent reduction in fibrotic lesions.
Significantly suppressed the BLM- induced overexpression of fibrotic markers such as FN, COL-I, and α-SMA, with the most pronounced effect observed at a dose of 10 mg/kg.
分子量

471.53

Formula

C26H26FN7O
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

Phosphodiesterase-IN-5 相关分类

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  • 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:

Phosphodiesterase-IN-5Phosphodiesterase (PDE)PKAInterleukin RelatedTNF ReceptorCollagenProtein kinase AILTumor Necrosis Factor ReceptorTNFRphosphodiesteraseBleomycinpulmonary fibrosisCREBcAMPInhibitorinhibitorinhibit

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