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Technical Data
| Formula | C25H20N4O |
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| Molecular Weight | 392.45 | CAS No. | 1292799-56-4 | |
| Solubility (25°C)* | In vitro | DMSO | 79 mg/mL (201.29 mM) | |
| Ethanol | 79 mg/mL (201.29 mM) | |||
| Water | Insoluble | |||
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* <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.) |
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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. | ||
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| 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: |
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References
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Customer Product Validation
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Data from [Oncogene, 2014, 10.1038/onc.2014.94]
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Data from [Oncogene, 2014, 10.1038/onc.2014.94]
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Data from [Data independently produced by , , Am J Hum Genet, 2017, 100(1):5-20]
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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 |
RETURN POLICY
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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.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.