PF-2545920


Catalog No. size PriceQuantity
M6450-2 2mg solid $120
M6450-10 10mg solid $482

Description

Cas:898562-94-2

Product Information

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.

 

Chemical Formula: C25H20N4O

 

Exact Mass: 392.16371

 

Molecular Weight: 392.0 

 

Elemental Analysis: C, 76.51; H, 5.14; N, 14.28; O, 4.08

 

Synonym: 

 

PF-2545920

PF 2545920

PF2545920

MP-10

MP10

MP 10, Mardepodect

 

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

 

InChi Key:

AZEXWHKOMMASPA-UHFFFAOYSA-N

 

InChi Code:  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

 

Smiles Code:

CN1N=C(C2=CC=C(OCC3=NC4=CC=CC=C4C=C3)C=C2)C(C5=CC=NC=C5)=C1

 

 

Technical Data:

 

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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.

 

  1. 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.

 

  1. 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.

 

  1. Uthayathas S, Masilamoni GJ, Shaffer CL, Schmidt CJ, Menniti FS, Papa SM. Phosphodiesterase 10A inhibitor MP-10 effects in primates: comparison with risperidone and mechanistic implications. Neuropharmacology. 2014 Feb;77:257-67. PubMed PMID: 24490227; PubMed Central PMCID: PMC3934827.

 

  1. Bleickardt CJ, Kazdoba TM, Jones NT, Hunter JC, Hodgson RA. Antagonism of the adenosine A2A receptor attenuates akathisia-like behavior induced with MP-10 or aripiprazole in a novel non-human primate model. Pharmacol Biochem Behav. 2014 Mar;118:36-45. doi: 10.1016/j.pbb.2013.10.030. Epub 2013 Nov 8. PubMed PMID: 24211858.

 

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

 

Payment & Security

American Express Apple Pay Diners Club Discover Elo Google Pay JCB Mastercard PayPal Shop Pay Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed