2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. PDE4-IN-32

PDE4-IN-32 (Compound B05) 是一种具有血脑屏障通透性的选择性 PDE4B 和 PDE4D 抑制剂，对二者的 IC50 值分别为 13.7 nM 和 23.8 nM。PDE4-IN-32 可促进 MCAO/R 小鼠模型的运动和认知功能恢复。PDE4-IN-32 可减轻脑水肿。PDE4-IN-32 可用于缺血性脑卒中的研究。

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PDE4-IN-32

PDE4-IN-32 Chemical Structure

CAS No. : 3080627-61-5

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PDE4-IN-32 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-32 (Compound B05) is a selective, blood-brain barrier permeable PDE4B and PDE4D inhibitor with IC50 values of 13.7 nM and 23.8 nM, respectively. PDE4-IN-32 promotes the recovery of motor and cognitive function in MCAO/R mouse models. PDE4-IN-32 reduces cerebral edema. PDE4-IN-32 can be used for the research of ischemic stroke[1].

IC50 & Target[1]

PDE4B

13.7 nM (IC50)

PDE4D

23.8 nM (IC50)

体外研究
(In Vitro)

PDE4-IN-32 可强效且选择性地抑制 PDE4 亚型，对 PDE4D 的 IC50 为 23.8 nM，对 PDE4B 的 IC50 为 13.7 nM，对其他 PDE 亚型的选择性超过 420 倍[1]。
PDE4-IN-32 (0.156-1.25 μM; 1 h) 可呈剂量依赖性地保护 HT-22 小鼠海马神经元细胞免受 OGD/R 诱导的损伤[1]。

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

PDE4-IN-32 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route MRT0-t MRT0-∞ T1/2 Vz/F CLz/F Cmax Tmax Bioavailability
Rat[1] 2.0 mg/kg i.v. 2.12 ± 0.12 h 2.16 ± 0.11 h 3.06 ± 0.64 h 12.67 ± 3.2 L/kg 2.91 ± 0.69 L/h/kg 645.83 ± 147.20 μg/L / /
Rat[1] 20 mg/kg p.o. 8.76 ± 0.46 h 9.00 ± 0.52 h 3.14 ± 0.44 h 88.18 ± 28.95 L/kg 19.17 ± 4.55 L/h/kg 105.03 ± 41.59 μg/L 8.0 ± 0 h 15.5 %
体内研究
(In Vivo)

PDE4-IN-32 (60 mg/kg；口服；单次剂量) 不会在成年雄性比格犬中引发呕吐[1]。
PDE4-IN-32 (2-30 mg/kg；腹腔注射) 可减小雄性 C57BL/6 小鼠在 MCAO/R 模型中的脑梗死体积，并以剂量依赖的方式减轻其脑梗死范围[1]。

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

Animal Model: C57BL/6 mice (8-week-old male, middle cerebral artery occlusion and reperfusion)[1]
Dosage: 2 mg/kg; 10 mg/kg; 30 mg/kg
Administration: i.p.; single dose at reperfusion
Result: Did not significantly reduce infarct volume at 2 mg/kg dose.
Reduced corrected infarct volume to 26.26 ± 6.15% (vs 42.34 ± 2.32% in vehicle controls, p < 0.001) and increased ipsilateral/contralateral ADC ratio to 74.03 ± 2.317% (vs 67.36 ± 4.535% in vehicle controls, p < 0.05) at 10 mg/kg dose.
Reduced corrected infarct volume to 17.82 ± 2.994% (vs vehicle, p < 0.0001) and increased ipsilateral/contralateral ADC ratio to 81.96 ± 3.862% (vs vehicle, p < 0.0001; vs 10 mg/kg dose, p < 0.05) at 30 mg/kg dose.
分子量

320.34

Formula

C20H16O4
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-32 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:

PDE4-IN-323080627-61-5Phosphodiesterase (PDE)astrocytesPDE4DMCAO/Rneuronal apoptosisPDE4Bcerebral edemaischemic strokeHT-22 mouse hippocampal neuronal cellsmicrogliablood-brain barrierInhibitorinhibitorinhibit

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