PDE4-IN-32
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3080627-61-5
- 分子式: C20H16O4
- 分子量:320.34
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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PDE4B 13.7 nM (IC50) |
PDE4D 23.8 nM (IC50) |
PDE4-IN-32 potently and selectively inhibits PDE4 isoforms, with an IC50 of 23.8 nM against PDE4D and 13.7 nM against PDE4B, and exhibits over 420-fold selectivity over other PDE isoforms[1].
PDE4-IN-32 (0.156-1.25 μM; 1 h) dose-dependently protects HT-22 mouse hippocampal neuron cells against OGD/R-induced injury[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| 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 % |
PDE4-IN-32 (2-30 mg/kg; i.p.) reduces cerebral infarct volume, attenuates cerebral infarct size in a dose-dependent manner in male C57BL/6 mice subjected to MCAO/R[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (8-week-old male, middle cerebral artery occlusion and reperfusion)[1]
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Dosage:2 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:i.p.; single dose at reperfusion
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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.
化学情報
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CAS 番号 3080627-61-5
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分子量 320.34
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分子式 C20H16O4
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SMILES
COC1=C2C(C=C(O2)C3CC3)=C(C=C1)C4=CC=C5C(OCC5=C4)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PDE4-IN-32 関連分類
HY-181549 関連分類
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