PF-2545920

PF-2545920, also known as Mardepodect, is a phosphodiesterase inhibitor selective for the PDE10A subtype, which 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. PDE10A inhibitors have shown behavioral effects in rodent models that predict antipsychotic efficacy. 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.

Product information

CAS Number: 898562-94-2

Molecular Weight: 392.45

Formula: C25H20N4O

Synonym:

MP-10

Mardepodect

PF-2545920

PF 2545920

PF2545920

MP10

MP 10, Mardepodect

Chemical Name: 2-(4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)phenoxymethyl)quinoline

Smiles: CN1C=C(C(=N1)C1C=CC(=CC=1)OCC1=CC=C2C=CC=CC2=N1)C1C=CN=CC=1

InChiKey: AZEXWHKOMMASPA-UHFFFAOYSA-N

InChi: InChI=1S/C25H20N4O/c1-29-16-23(18-12-14-26-15-13-18)25(28-29)20-7-10-22(11-8-20)30-17-21-9-6-19-4-2-3-5-24(19)27-21/h2-16H,17H2,1H3

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vivo:

In the conditioned avoidance response assay (CAR), PF-2545920 is active with an ED50 of 1 mg/kg. Administration of PF-2545920 to mice causes a dose dependent increase in striatal cGMP.

References:

1. Hamaguchi W, Masuda N, Samizu K, Mihara T, Takama K, Watanabe T.Synthesis and in vivo evaluationof novel quinoline derivatives as phosphodiesterase 10A inhibitors. Chem Pharm Bull (Tokyo). 2014;62(12):1200-13. PubMed PMID: 25450629.
2. Lin SF, Labaree D, Chen MK, Holden D, Gallezot JD, Kapinos M, Teng JK, Najafzadeh S, Plisson C, Rabiner EA, Gunn RN, Carson RE, Huang Y. Further evaluation of [11C]MP-10 as a radiotracer for phosphodiesterase 10A: PET imaging study in rhesus monkeys and brain tissue metabolite analysis. Synapse. 2015 Feb;69(2):86-95. doi: 10.1002/syn.21792. Epub 2014 Dec 11. PubMed PMID: 25450608; PubMed Central PMCID: PMC4275380.
3. Natesan S, Ashworth S, Nielsen J, Tang SP, Salinas C, Kealey S, Lauridsen JB, Stensbøl TB, Gunn RN, Rabiner EA, Kapur S. Effect of chronic antipsychotic treatment on striatal phosphodiesterase 10A levels: a [¹¹C]MP-10 PET rodent imaging study with ex vivo confirmation. Transl Psychiatry. 2014 Apr 1;4:e376. doi: 10.1038/tp.2014.17. PubMed PMID: 24690597; PubMed Central PMCID: PMC4012281.

Products are for research use only. Not for human use.