WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H462479
CAS#: 2070014-78-5 (HCl)
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#: H462479
Name: Mardepodect HCl
CAS#: 2070014-78-5 (HCl)
Chemical Formula: C25H21ClN4O
Exact Mass: 428.14
Molecular Weight: 428.920
Elemental Analysis: C, 70.01; H, 4.94; Cl, 8.26; N, 13.06; O, 3.73
Related CAS #: 1292799-56-4 898562-94-2 (free base) 2070014-78-5 (HCl) 898563-49-0 (succinate)
Synonym: Mardepodect hydrochloride; PF-2545920 hydrochloride; PF2545920 HCl; PF 2545920; PF-2545920; PF2545920;
IUPAC/Chemical Name: 2-((4-(1-methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl)phenoxy)methyl)quinoline hydrochloride
InChi Key: BDHTXAXWOXYUDG-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H20N4O.ClH/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;1H
SMILES Code: CN1N=C(C2=CC=C(OCC3=NC4=CC=CC=C4C=C3)C=C2)C(C5=CC=NC=C5)=C1.Cl[H]
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
Shelf Life: >3 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 428.92 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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1: Wilson JM, Ogden AM, Loomis S, et al. Phosphodiesterase 10A inhibitor, MP-10 (PF-2545920), produces greater induction of c-Fos in dopamine D2 neurons than in D1 neurons in the neostriatum. Neuropharmacology. 2015;99:379-386. doi:10.1016/j.neuropharm.2015.08.008
2: Verhoest PR, Chapin DS, Corman M, 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. doi:10.1021/jm900521k