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Mardepodect

Catalog No. T16499 CAS 898562-94-2

Synonyms: PF-2545920

Mardepodect (PF-2545920) is a phosphodiesterase inhibitor selective for the PDE10A subtype with an IC50 of 0.37 nM, <1000-fold selectivity over PDE. It is potentially useful for the treatment of schizophrenia. Phosphodiesterase 10A (PDE10A) is highly expressed in striatal medium spiny neurons of both the direct and indirect output pathways. Mardepodect can cross the blood-brain barrier.

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Mardepodect, CAS 898562-94-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
2 mg	In stock	$ 50.00
5 mg	In stock	$ 84.00
10 mg	In stock	$ 153.00
25 mg	In stock	$ 258.00
50 mg	In stock	$ 385.00
100 mg	In stock	$ 576.00
1 mL * 10 mM (in DMSO)	In stock	$ 93.00

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Purity: 99.81%

Purity: 98.82%

Biological Description

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Storage & Solubility Information

Description	Mardepodect (PF-2545920) is a phosphodiesterase inhibitor selective for the PDE10A subtype with an IC50 of 0.37 nM, >1000-fold selectivity over PDE. It is potentially useful for the treatment of schizophrenia. Phosphodiesterase 10A (PDE10A) is highly expressed in striatal medium spiny neurons of both the direct and indirect output pathways. Mardepodect can cross the blood-brain barrier.
Targets&IC50	PDE10A:0.37 nM
In vivo	Mardepodect is active in a range of antipsychotic models with the ED50 of 1 mg/kg, 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.Mardepodect induces a dose-dependent increase in striatal cGMP in mice.

Synonyms	PF-2545920
Molecular Weight	392.45
Formula	C25H20N4O
CAS No.	898562-94-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (114.66 mM)

References and Literature

1. 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, 2009, 52(16), 5188-5196. 2. Grauer SM, et al. Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia. J Pharmacol Exp Ther, 2009, 331(2), 574-590.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library NO PAINS Compound Library Clinical Compound Library Bioactive Compounds Library Max Bioactive Compound Library Orally Active Compound Library Metabolism Compound Library Human Metabolite Library

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Keywords

Mardepodect 898562-94-2 Metabolism PDE PF-02545920 inhibit PF 2545920 PF-2545920 Inhibitor Phosphodiesterase (PDE) PF2545920 inhibitor

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