WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H522364
CAS#: 898562-94-2 (free base)
Description: Mardepodect, also known as PF-2545920, 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.
Hodoodo Cat#: H522364
Name: Mardepodect free base
CAS#: 898562-94-2 (free base)
Chemical Formula: C25H20N4O
Exact Mass: 392.16
Molecular Weight: 392.462
Elemental Analysis: C, 76.51; H, 5.14; N, 14.28; O, 4.08
Related CAS #: 1292799-56-4 898562-94-2 (free base) 2070014-78-5 (HCl) 898563-49-0 (succinate)
Synonym: PF-2545920; PF 2545920; PF2545920; MP-10; MP10; MP 10, Mardepodect;
IUPAC/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
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
More Info:
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The following data is based on the product molecular weight 392.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
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| In vivo protocol: |
1: Hamaguchi W, Masuda N, Samizu K, Mihara T, Takama K, Watanabe T. Synthesis and in vivo evaluation of 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.
4: 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.
5: 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.
6: Piccart E, Langlois X, Vanhoof G, D'Hooge R. Selective inhibition of phosphodiesterase 10A impairs appetitive and aversive conditioning and incentive salience attribution. Neuropharmacology. 2013 Dec;75:437-44. doi: 10.1016/j.neuropharm.2013.08.006. Epub 2013 Aug 22. PubMed PMID: 23973318.
7: Meslamani J, Bhajun R, Martz F, Rognan D. Computational profiling of bioactive compounds using a target-dependent composite workflow. J Chem Inf Model. 2013 Sep 23;53(9):2322-33. doi: 10.1021/ci400303n. Epub 2013 Aug 26. PubMed PMID: 23941602.
8: Hu E, Ma J, Biorn C, Lester-Zeiner D, Cho R, Rumfelt S, Kunz RK, Nixey T, Michelsen K, Miller S, Shi J, Wong J, Hill Della Puppa G, Able J, Talreja S, Hwang DR, Hitchcock SA, Porter A, Immke D, Allen JR, Treanor J, Chen H. Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer. J Med Chem. 2012 May 24;55(10):4776-87. doi: 10.1021/jm3002372. Epub 2012 May 11. PubMed PMID: 22548439.
9: Plisson C, Salinas C, Weinzimmer D, Labaree D, Lin SF, Ding YS, Jakobsen S, Smith PW, Eiji K, Carson RE, Gunn RN, Rabiner EA. Radiosynthesis and in vivo evaluation of [(11)C]MP-10 as a positron emission tomography radioligand for phosphodiesterase 10A. Nucl Med Biol. 2011 Aug;38(6):875-84. doi: 10.1016/j.nucmedbio.2011.02.005. Epub 2011 Mar 30. PubMed PMID: 21843784.
10: Dedeurwaerdere S, Wintmolders C, Vanhoof G, Langlois X. Patterns of brain glucose metabolism induced by phosphodiesterase 10A inhibitors in the mouse: a potential translational biomarker. J Pharmacol Exp Ther. 2011 Oct;339(1):210-7. doi: 10.1124/jpet.111.182766. Epub 2011 Jul 8. PubMed PMID: 21742809.
11: Tu Z, Fan J, Li S, Jones LA, Cui J, Padakanti PK, Xu J, Zeng D, Shoghi KI, Perlmutter JS, Mach RH. Radiosynthesis and in vivo evaluation of [11C]MP-10 as a PET probe for imaging PDE10A in rodent and non-human primate brain. Bioorg Med Chem. 2011 Mar 1;19(5):1666-73. doi: 10.1016/j.bmc.2011.01.032. Epub 2011 Jan 22. PubMed PMID: 21315609; PubMed Central PMCID: PMC3056285.
12: Torremans A, Ahnaou A, Van Hemelrijck A, Straetemans R, Geys H, Vanhoof G, Meert TF, Drinkenburg WH. Effects of phosphodiesterase 10 inhibition on striatal cyclic AMP and peripheral physiology in rats. Acta Neurobiol Exp (Wars). 2010;70(1):13-9. PubMed PMID: 20407482.
13: Zhang HT. Phosphodiesterase Targets for Cognitive Dysfunction and Schizophrenia--a New York Academy of Sciences Meeting. IDrugs. 2010 Mar;13(3):166-8. PubMed PMID: 20191432.
14: Grauer SM, Pulito VL, Navarra RL, Kelly MP, Kelley C, Graf R, Langen B, Logue S, Brennan J, Jiang L, Charych E, Egerland U, Liu F, Marquis KL, Malamas M, Hage T, Comery TA, Brandon NJ. Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia. J Pharmacol Exp Ther. 2009 Nov;331(2):574-90. doi: 10.1124/jpet.109.155994. Epub 2009 Aug 6. PubMed PMID: 19661377.
15: Verhoest PR, Chapin DS, Corman M, Fonseca K, Harms JF, Hou X, Marr ES, Menniti FS, Nelson F, O'Connor R, Pandit J, Proulx-Lafrance C, Schmidt AW, Schmidt CJ, Suiciak JA, Liras S. 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 Aug 27;52(16):5188-96. doi: 10.1021/jm900521k. PubMed PMID: 19630403.
