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.
For research use only. We do not sell to patients.
- CAS No.: 3080627-61-5
- Formula: C20H16O4
- Molecular Weight:320.34
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Storage:
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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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PDE4B 13.7 nM (IC50) |
PDE4D 23.8 nM (IC50) |
In Vitro
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. Further protocols information, click here.
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 % |
In Vivo
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.
Chemical Information
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CAS No. 3080627-61-5
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Molecular Weight 320.34
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Water Maze
The Morris Water Maze is a rodent spatial learning and memory assay in which a mouse or rat swims in opaque water to find an escape platform; in the hidden-platform version, the animal cannot see the platform and must use distal extra-maze cues to learn its fixed spatial location. The assay primarily measures hippocampus-dependent spatial learning during acquisition trials and spatial reference memory during probe trials after platform removal; readouts include escape latency, swim path length, swim speed, quadrant occupancy, platform-site crossings, and proximity to the former platform location.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PDE4-IN-32 Related Classifications
HY-181549 Related Classifications
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