Mardepodect HCl
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MedKoo CAT#: 462479

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.


Chemical Structure

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Mardepodect HCl
CAS# 2070014-78-5 (HCl)

Theoretical Analysis

MedKoo Cat#: 462479
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

Price and Availability

Size Price Availability Quantity
5mg USD 385 2 Weeks
10mg USD 650 2 Weeks
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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:

Product Data:
Biological target: Mardepodect hydrochloride (PF-2545920 hydrochloride) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs.
In vitro activity: Subsequent western blot and reverse transcription polymerase chain reaction analyses showed that MP-10 reduced the mRNA and protein levels of inducible nitric oxide synthase, cyclooxygenase-2, proinflammatory cytokines, and matrix metalloproteinase-3, -8, and - 9 in LPS-stimulated BV2 cells. Further mechanistic studies revealed that MP-10 exerts anti-inflammatory effects by inhibiting the phosphorylation of c-Jun N-terminal kinase and Akt, reducing the activity of nuclear factor-kappa B/activator protein-1, and upregulating the nuclear factor erythroid 2-related factor 2/antioxidant response element and protein kinase A/cAMP response element-binding protein signaling pathways. Reference: J Neuroimmune Pharmacol. 2021 Jun;16(2):470-482. https://pubmed.ncbi.nlm.nih.gov/32671618/
In vivo activity: MP-10 (1, 3, 10 or 30 mg/kg, PO) dose-dependently increased c-Fos immunopositive nuclei in all regions of neostriatum. In the Drd1a-tdTomato mice, MP-10 (3 or 10 mg/kg, IP) increased c-Fos immunoreactivity in both types of neurons, the induction was greater in the D1-negative neurons. Reference: Neuropharmacology. 2015 Dec;99:379-86. https://pubmed.ncbi.nlm.nih.gov/26256420/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 25.0 58.29

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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: 1. Kim DY, Park JS, Leem YH, Park JE, Kim HS. The Potent PDE10A Inhibitor MP-10 (PF-2545920) Suppresses Microglial Activation in LPS-Induced Neuroinflammation and MPTP-Induced Parkinson's Disease Mouse Models. J Neuroimmune Pharmacol. 2021 Jun;16(2):470-482. doi: 10.1007/s11481-020-09943-6. Epub 2020 Jul 15. PMID: 32671618. 2. Hankir MK, Kranz M, Gnad T, Weiner J, Wagner S, Deuther-Conrad W, Bronisch F, Steinhoff K, Luthardt J, Klöting N, Hesse S, Seibyl JP, Sabri O, Heiker JT, Blüher M, Pfeifer A, Brust P, Fenske WK. A novel thermoregulatory role for PDE10A in mouse and human adipocytes. EMBO Mol Med. 2016 Jul 1;8(7):796-812. doi: 10.15252/emmm.201506085. PMID: 27247380; PMCID: PMC4931292. 3. Chen J, Zook D, Crickard L, Tabatabaei A. Effect of phosphodiesterase (1B, 2A, 9A and 10A) inhibitors on central nervous system cyclic nucleotide levels in rats and mice. Neurochem Int. 2019 Oct;129:104471. doi: 10.1016/j.neuint.2019.104471. Epub 2019 May 20. PMID: 31121256. 4. Wilson JM, Ogden AM, Loomis S, Gilmour G, Baucum AJ 2nd, Belecky-Adams TL, Merchant KM. 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 Dec;99:379-86. doi: 10.1016/j.neuropharm.2015.08.008. Epub 2015 Aug 7. PMID: 26256420.
In vitro protocol: 1. Kim DY, Park JS, Leem YH, Park JE, Kim HS. The Potent PDE10A Inhibitor MP-10 (PF-2545920) Suppresses Microglial Activation in LPS-Induced Neuroinflammation and MPTP-Induced Parkinson's Disease Mouse Models. J Neuroimmune Pharmacol. 2021 Jun;16(2):470-482. doi: 10.1007/s11481-020-09943-6. Epub 2020 Jul 15. PMID: 32671618. 2. Hankir MK, Kranz M, Gnad T, Weiner J, Wagner S, Deuther-Conrad W, Bronisch F, Steinhoff K, Luthardt J, Klöting N, Hesse S, Seibyl JP, Sabri O, Heiker JT, Blüher M, Pfeifer A, Brust P, Fenske WK. A novel thermoregulatory role for PDE10A in mouse and human adipocytes. EMBO Mol Med. 2016 Jul 1;8(7):796-812. doi: 10.15252/emmm.201506085. PMID: 27247380; PMCID: PMC4931292.
In vivo protocol: 1. Chen J, Zook D, Crickard L, Tabatabaei A. Effect of phosphodiesterase (1B, 2A, 9A and 10A) inhibitors on central nervous system cyclic nucleotide levels in rats and mice. Neurochem Int. 2019 Oct;129:104471. doi: 10.1016/j.neuint.2019.104471. Epub 2019 May 20. PMID: 31121256. 2. Wilson JM, Ogden AM, Loomis S, Gilmour G, Baucum AJ 2nd, Belecky-Adams TL, Merchant KM. 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 Dec;99:379-86. doi: 10.1016/j.neuropharm.2015.08.008. Epub 2015 Aug 7. PMID: 26256420.

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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