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Description
Overview
A cell-permeable pyrazolocarboxylic acid that acts as a selective D-amino acid oxidase (DAO/DAAO/DAMOX/OXDA) inhibitor (IC50 = 910 nM against human DAO; [D-ser] = 10 mM) and effectively protects DAO overexpressing cultures from oxidative stress-induced cell death upon D-Ser (50 mM) exposure (ED50 ≤3.95 µM), while exhibiting little affinity toward NMDAR glycine binding site or inhibitory activity against D-aspartate oxidase (DDO/DSOX). Reported to be orally available and blood-brain barrier-permeant in rats and effectively prevent PCP (phencyclidine) from suppressing PPI (prepulse inhibition) response in mice (single 80 mg/kg or 56X 20 mg/kg/12 h b.i.d. oral dosages) in vivo.
Catalogue Number
251406
Brand Family
Calbiochem®
Synonyms
5-methyl-1H-pyrazole-3-carboxylic acid, DAAO Inhibitor III
References
References
Smith, S., et al. 2010. Open Med. Chem. J.27, 3. Williams, M. 2009. Biochem. Pharmacol.78, 1360. Adage, T., et al. 2008. Eur. Neuropsychopharmacol.18, 200.
Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity
Standard Handling
Storage
+2°C to +8°C
Protect from Light
Protect from light
Do not freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas
Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Documentation
Références bibliographiques
Aperçu de la référence bibliographique
Smith, S., et al. 2010. Open Med. Chem. J.27, 3. Williams, M. 2009. Biochem. Pharmacol.78, 1360. Adage, T., et al. 2008. Eur. Neuropsychopharmacol.18, 200.
Fiche technique
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
08-March-2013 JSW
Synonyms
5-methyl-1H-pyrazole-3-carboxylic acid, DAAO Inhibitor III
Description
A cell-permeable pyrazolocarboxylic acid that acts as a selective D-amino acid oxidase (DAO/DAAO/DAMOX/OXDA) inhibitor (IC50 = 910 nM against human DAO; [D-ser] = 10 mM) and effectively protects DAO overexpressing cultures from oxidative stress-induced cell death upon D-Ser (50 mM) exposure (ED50 ≤3.95 µM), while exhibiting little affinity toward NMDAR glycine binding site (6% inhibition at 100 µM), nor inhibitory activity against D-aspartate oxidase (DDO/DSOX; 43% inhibition at 100 µM) or serine racemase (no inhibition at 50 µM). AS057278 is orally available (plasma Cmax = 8.089 µg/mL; t1/2 = 7.21 h; tmax = 1 h post 10 mg/mL oral dosing in rats) and can cross blood-brain barrier (1.622 and 0.578 µg/g brain tissue, respectively, 15 and 60 min post single 10 mg/kg i.v. dosing in rats). Effectively prevents PCP (phencyclidine) from suppressing PPI (prepulse inhibition; prepulse noise = 82 dB, startle noise = 120 dB) response in mice via either long-term oral administration (93% and 70% of no-PCP control PPI level, respectively, with or without 28-day b.i.d, treatment at 20 mg/kg/12 h) or single acute heavy oral dosing (93% and 53% of no-PCP control PPI level, respectively, with or without 80 mg/kg dosing) 60 min prior to PCP treatment (8 mg/kg i.p.) in vivo.
Form
White solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
402-61-9
Chemical formula
C₅H₆N₂O₂
Structure formula
Purity
≥99% by HPLC
Solubility
DMSO (50 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Smith, S., et al. 2010. Open Med. Chem. J.27, 3. Williams, M. 2009. Biochem. Pharmacol.78, 1360. Adage, T., et al. 2008. Eur. Neuropsychopharmacol.18, 200.
