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513050 Sigma-Aldrich

PDE10A Inhibitor, Cpd15 - Calbiochem

Synonym: (6-chloro-3,8-dimethyl-1H-pyrazolo[3,4-b]quinolin-4-yl)(2-methylpyrimidin-5-yl)methanol, Phosphodiesterase 10A Inhibitor, PDE10A Inhibitor, Cpd15 - Calbiochem

  • Empirical Formula (Hill Notation) C18H16ClN5O

  • Molecular Weight 353.81

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Properties

Related Categories Cell Biology, Cell Signaling and Neuroscience, Cyclic Nucleotide Metabolism, G Proteins and Cyclic Nucleotides, Phosphodiesterase Inhibitors More...
Quality Level   100
assay   ≥98% (HPLC)
form   powder
potency   ≤5 nM Ki
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   +2C to +8C
color   off-white
solubility   DMSO: 100 mg/mL
shipped in   wet ice

Description

General description

A cell-permeable pyrazoloquinoline compound that acts as a potent phosphodiesterase 10A inhibitor (Ki≤5 nM against human PDE10A), while exhibiting >500-fold selectivity over other human PDEs 1-11 and little activity against CYP3A4 (IC50 >20 µM) or a panel of 23 kinases (IC50 >30 µM). Reported to be orally available in monkey and rat species and be efficacious in reversing NMDAR antagonist (+)-MK-801- (Cat. No. 475878) induced hyperactivity in a ratsl (MED = 10 mg/kg p.o.) in vivo.

A cell-permeable pyrazoloquinoline compound that acts as a potent phosphodiesterase 10A inhibitor (Ki≤5 nM against human PDE10A-catalyzed cAMP hydrolysis), while exhibiting >500-fold selectivity over other human PDEs 1-11 and much reduced or little activity against CYP3A4 (IC50 = 7.9 and >20 µM, respectively, with or without preincubation) as well as a panel of 23 kinases (IC50 >30 µM). Reported to be orally available in monkey (AUC0-6 h = 11,496 nM·h, T1/2 = 7.1 h; 3 mg/kg p.o.) and rat (AUC0-6 h475878) induced hyperactivity (1 h post p.o.) in a rat schizophrenia model (MED = 10 mg/kg p.o.) in vivo.

Packaging

5 mg in Glass bottle

Biochem/physiol Actions

Cell permeable: yes

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

McElroy, W., et al. 2012. Bioorg. Med. Chem. Lett.22, 1335.

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
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