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D159687 is a selective negative allosteric modulator (NAM) of PDE4D. D159687 induces a transient increase in CREB phosphorylation which peaked at 6 hours after treatment. D159687 causes optimal CREB phosphorylation at 1 μM.
In vivo, D159687 (0.05-5 mg/kg; oral daily for a week) shows a potential recruitment or enhancement of synaptic function with increased task difficulty in female Cynomolgus macaques.
| Cell Experiment | |
|---|---|
| Cell lines | HT-22 cells |
| Preparation method | cAMP concentrations were measured using the enzyme-linked immunosorbent assay (ELISA). On the day of treatment, the attached HT-22 cells were washed with warm phosphate buffer saline (PBS) and then incubated for 10 min with PBS supplemented with various concentrations of D159687 and further for 10 min with 10 nM isoproterenol in the system52. After incubation, PBS containing the drugs was removed and the plates were let dry roughly before 200 μl HCl (0.1 M) was added to each well to lyse the cells. Cell lysates were collected into Eppendorf tubes and centrifuged at 800 × g for 15 min. Supernatants were collected for immediate assay or stored frozen for assay later using the cAMP complete ELISA kit (Enzo Life Sciences, Farmingdale, NY) according to the assay protocol. |
| Concentrations | 0.1 and 1 μM |
| Incubation time | - |
| Animal Experiment | |
|---|---|
| Animal models | Female Cynomolgus macaques (4-6 years; weights 2.39-3.6 Kg) |
| Formulation | prepared as solutions in a 0.5% (w/v) Poloxamer 188: 0.5% (w/v) HPMC: 0.4% Tween 80 vehicle at 5.0 mg/mL |
| Dosages | 0.05, 0.5 and 5.0 mg/Kg |
| Administration | PO gavage |
| Molecular Weight | 366.84 |
| Formula | C21H19ClN2O2 |
| CAS Number | 1155877-97-6 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PDE Products |
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MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 μM. |
| MMPX
MMPX is a potent PDE1 inhibitor. |
| T-0156
T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. |
| TPN171
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| Mesopram
Mesopram (Daxalipram) is an orally active phosphodiesterase (PDE) 4 inhibitor. |
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