PF-2545920
| Code | Size | Price |
|---|
| AG-CR1-3636-M001 | 1 mg | £55.00 |
Quantity:
| AG-CR1-3636-M005 | 5 mg | £145.00 |
Quantity:
| AG-CR1-3636-M025 | 25 mg | £400.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
-20°C
Storage:
Short Term: 4°C Long Term: -20°C
Documents
Further Information
Alternate Names/Synonyms:
2-(4-(1-Methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl)-phenoxymethyl)quinoline; MP-10
Appearance:
Solid.
CAS:
898562-94-2
EClass:
32160000
Form (Short):
liquid
GHS Symbol:
GHS07
Handling Advice:
Keep cool and dry.
Hazards:
H302, H319
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
InChiKey:
AZEXWHKOMMASPA-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 898562-94-2. Formula: C25H20N4O. MW: 392.5. Potent and selective phosphodiesterase 10A (PDE10A) inhibitor (IC50=1.26nM) in vitro and in vivo. PDE10A is a cGMP and cAMP degrading PDE isozyme with neurological importance and was shown to be implicated in the regulation of energy homeostasis. Inhibition of PDE10A leads to interference of the breakdown of the secondary messenger cAMP and cGMP. Anti-psychotic agent. Useful for the treatment of schizophrenia. Anticancer agent. Inhibits colon tumor cell growth for which high levels of PDE10A have been reported. Antiobesity and antidiabetic agent. Induces browning in white adipose tissue (WAT).
MDL:
MFCD09743765
Molecular Formula:
C25H20N4O
Molecular Weight:
392.5
Package Type:
Vial
Precautions:
P280, P301, P312, P305, P351, P338, P337, P313
Product Description:
Potent and selective phosphodiesterase 10A (PDE10A) inhibitor (IC50=1.26nM) in vitro and in vivo. PDE10A is a cGMP and cAMP degrading PDE isozyme with neurological importance and was shown to be implicated in the regulation of energy homeostasis. Inhibition of PDE10A leads to interference of the breakdown of the secondary messenger cAMP and cGMP. Anti-psychotic agent. Useful for the treatment of schizophrenia. Anticancer agent. Inhibits colon tumor cell growth for which high levels of PDE10A have been reported. Antiobesity and antidiabetic agent. Induces browning in white adipose tissue (WAT).
Purity:
>98% (HPLC)
Signal word:
Warning
SMILES:
CN(C=C1C2=CC=NC=C2)N=C1C(C=C3)=CC=C3OCC4=NC5=CC=CC=C5C=C4
Solubility Chemicals:
Soluble in DMSO or ethanol. Insoluble in water.
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C. Store solutions at -20°C in the dark.
References
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: P.R. Verhoest, et al.; J. Med. Chem. 52, 5188 (2009) | Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia: S.M. Grauer, et al.; J. Pharmacol. Exp. Ther. 331, 574 (2009) | Effects of phosphodiesterase 10 inhibition on striatal cyclic AMP and peripheral physiology in rats: A. Torremans, et al.; Acta Neurobiol. Exp. 70, 13 (2010) | Phosphodiesterase 10A inhibitor, MP-10 (PF-2545920), produces greater induction of c-Fos in dopamine D2 neurons than in D1 neurons in the neostriatum: J.M. Wilson, et al.; Neuropharmacol. 99, 379 (2015) | beta-catenin nuclear translocation in colorectal cancer cells is suppressed by PDE10A inhibition, cGMP elevation, and activation of PKG: K. Lee, et al.; Oncotarget 7, 5353 (2016) | A novel thermoregulatory role for PDE10A in mouse and human adipocytes: M.K. Hankir, et al.; EMBO Mol. Med. 8, 796 (2016)
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