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| 25mg |
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Purity: ≥98%
Mardepodect HCl, the hydrochloric acid salt of PF-2545920 (Also known as Mardepodect, MP-10), is a novel, potent and selective PDE10A (phosphodiesterase) inhibitor with IC50 of 0.37 nM, and with >1000-fold selectivity over the PDE. It is potentially useful for the treatment of schizophrenia. PF-2545920 is active in a range of antipsychotic models, antagonizing apomorphine-induced climbing in mice, inhibiting conditioned avoidance responding in both rats and mice, and blocking N-methyl-D-aspartate antagonist-induced deficits in prepulse inhibition of acoustic startle response in rats, while improving baseline sensory gating in mice.
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| ln Vivo |
With an ED50 of 1 mg/kg, mardepodect (PF-2545920) is active in the conditioned avoidance response (CAR). The striatal cGMP assay in mice administered Mardepodect (PF-2545920) increases in a dose-dependent manner[2].
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| References |
[1]. Wilson JM et al. Phosphodiesterase 10A inhibitor, MP-10 (PF-2545920), produces greater induction of c-Fos in D2 neurons than in D1 neurons in the neostriatum. Neuropharmacology. 2015 Dec;99:379-86.
[2]. Verhoest PR et al. Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. J Med Chem. |
| Molecular Formula |
C25H21CLN4O
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| Molecular Weight |
428.9134
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| CAS # |
2070014-78-5
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| Related CAS # |
898562-94-2
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| SMILES |
Cl[H].O(C([H])([H])C1C([H])=C([H])C2=C([H])C([H])=C([H])C([H])=C2N=1)C1C([H])=C([H])C(=C([H])C=1[H])C1C(C2C([H])=C([H])N=C([H])C=2[H])=C([H])N(C([H])([H])[H])N=1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3315 mL | 11.6575 mL | 23.3149 mL | |
| 5 mM | 0.4663 mL | 2.3315 mL | 4.6630 mL | |
| 10 mM | 0.2331 mL | 1.1657 mL | 2.3315 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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