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D159687

Cat. No. M10517
D159687 Structure
Synonym:

D-159687

Size Price Availability Quantity
5mg USD 425  USD425 In stock
10mg USD 720  USD720 In stock
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Biological Activity

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.

Protocol (for reference only)
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
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] David J Titus, et al. Neurobiol Learn Mem. A negative allosteric modulator of PDE4D enhances learning after traumatic brain injury

[2] Chong Zhang, et al. Sci Rep. Comparison of the Pharmacological Profiles of Selective PDE4B and PDE4D Inhibitors in the Central Nervous System

[3] Jane S Sutcliffe, et al. PLoS One. Efficacy of selective PDE4D negative allosteric modulators in the object retrieval task in female cynomolgus monkeys (Macaca fascicularis)

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  Catalog
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