Mardepodect (PF-2545920)

Catalog No.S2687 Batch:S268705

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Technical Data

Formula

C25H20N4O
Molecular Weight 392.45 CAS No. 1292799-56-4
Solubility (25°C)* In vitro DMSO 100 mg/mL (254.8 mM)
Ethanol 100 mg/mL (254.8 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.83mg/ml Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Mardepodect (PF-2545920) is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE.
Targets
PDE10A [2]
(Cell-free assay)
0.37 nM
In vitro PF-2545920 shows excellent potency and selectivity of PDE10A with IC50 of 1.26 nM. [1]
In vivo PF-2545920 intraperitoneally administrated at dose of 0.3, 3, and 5 mg/kg in male CF-1 mice causes striking increases in GluR1 phosphorylation levels of 3-, 5.4-, and 4.1-fold , respectively. MP-10 at concentration of 1 μM treats Rat striatal slices for 30 min, the level of GluR1S845 phosphorylation at the cell surface is significantly increased 2-fold, without change the level of total GluR1 on the cell surface. MP-10 intraperitoneally administrated at dose of 0.3, 3, and 5 mg/kg in male CF-1 mice results in robust, statistically significant increases in CREBS133 phosphorylation of 3-, 4-, and 2.6-fold, respectively. MP-10 intraperitoneally administrated at dose of 3 mg/kg increases both enkephalin and substance-P mRNA levels in striatum of CF-1 mice. MP-10 intraperitoneally administrated at dose of 0.3-1 mg/kg decreases avoidance responding with a significant treatment effect in the mouse CAR model. Mice treated with MP-10 at dose of 0.03 mg/kg spents more time in the empty than social side in the mice, MP-10 also dose-dependently decreased locomotor activity. [1] PDE10A subcutaneously administrated at dose of 1 mg/kg elevates striatal cGMP about 3 fold in male CD-1 mice, while PDE10A subcutaneously administrated at dose of 3.2 mg/kg displays a maximal elevation of striatal cGMP approximately a 5-fold increase in male CD-1 mice. PDE10A intravenous injected at a dose of 0.1 mg/kg in Sprague-Dawley rats displays clearance of 36 ml/min/Kg, DE10A intravenous injected at a dose of 0.3 mg/kg in Dog Beagle displays clearance of 7.2 ml/min/Kg in vivo clearance with a moderate volume of distribution, DE10A intravenous injected at a dose of 0.03 mg/kg in Monkey Cynomolgus displays clearance of 13.9 ml/min/Kg in vivo clearance with a moderate volume of distribution. PDE10A is active with an ED50 of 1 mg/kg at a significantly lower total plasma exposure (115 nM) in the conditioned avoidance response assay (CAR) in Sprague-Dawley rats. [2]

Protocol (from reference)

Animal Study:

[2]
  • Animal Models

    Jugular vein-cannulated male Sprague-Dawley rats

  • Dosages

    0.1 mg/kg

  • Administration

    Inject intravenous through jugular vein catheter in a single dose 4 hours before feed

Customer Product Validation

Data from [Oncogene, 2014, 10.1038/onc.2014.94]

Data from [Oncogene, 2014, 10.1038/onc.2014.94]

Data from [Data independently produced by , , Am J Hum Genet, 2017, 100(1):5-20]

Data from [Data independently produced by , , Front Mol Neurosci, 2017, 10:100]

Selleck's Mardepodect (PF-2545920) has been cited by 8 publications

Phosphodiesterase 10A (PDE10A) as a novel target to suppress β-catenin and RAS signaling in epithelial ovarian cancer [ J Ovarian Res, 2022, 15(1):120] PubMed: 36324187
The Potent PDE10A Inhibitor MP-10 (PF-2545920) Suppresses Microglial Activation in LPS-Induced Neuroinflammation and MPTP-Induced Parkinson's Disease Mouse Models [ J Neuroimmune Pharmacol, 2020, 10.1007/s11481-020-09943-6] PubMed: 32671618
Proteome-scale investigation of protein allosteric regulation perturbed by somatic mutations in 7,000 cancer genomes [Shen Q Am J Hum Genet, 2017, 100(1):5-20] PubMed: 27939638
Phosphodiesterase 10A is overexpressed in lung tumor cells and inhibitors selectively suppress growth by blocking β-catenin and MAPK signaling. [ Oncotarget, 2017, 8(41):69264-69280] PubMed: 29050202
The Phosphodiesterase 10A Inhibitor PF-2545920 Enhances Hippocampal Excitability and Seizure Activity Involving the Upregulation of GluA1 and NR2A in Post-synaptic Densities. [Zhang Y, et al. Front Mol Neurosci, 2017, 10:100] PubMed: 28439226
A novel thermoregulatory role for PDE10A in mouse and human adipocytes. [ EMBO Mol Med, 2016, 8(7):796-812] PubMed: 27247380
Luteinizing Hormone Causes Phosphorylation and Activation of the cGMP Phosphodiesterase PDE5 in Rat Ovarian Follicles, Contributing, Together with PDE1 Activity, to the Resumption of Meiosis [Egbert JR, et al. Biol Reprod, 2016, 94(5):110] PubMed: 27009040
Phosphodiesterase 10A: a novel target for selective inhibition of colon tumor cell growth and β-catenin-dependent TCF transcriptional activity. [Li N, et al. Oncogene, 2014, 10.1038/onc.2014.94] PubMed: 24704829

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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