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513050

Sigma-Aldrich

PDE10A Inhibitor, Cpd15

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C18H16ClN5O
Molecular Weight:
353.81
UNSPSC Code:
12352200

assay

≥98% (HPLC)

Quality Level

form

powder

potency

≤5 nM Ki

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 100 mg/mL

shipped in

wet ice

storage temp.

2-8°C

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.

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk_germany

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificates of Analysis (COA)

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