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251406 D-Amino Acid Oxidase Inhibitor III, AS057278 - CAS 402-61-9 - Calbiochem

251406
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Descripción

Replacement Information

Tabla espec. clave

Empirical FormulaCAS #
C₅H₆N₂O₂ 402-61-9

Products

Número de referenciaEmbalaje Cant./Env.
251406-50MG Frasco de vidrio 50 mg
Description
OverviewA 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 Number251406
Brand Family Calbiochem®
Synonyms5-methyl-1H-pyrazole-3-carboxylic acid, DAAO Inhibitor III
References
ReferencesSmith, 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.
Product Information
CAS number402-61-9
FormWhite solid
Hill FormulaC₅H₆N₂O₂
Chemical formulaC₅H₆N₂O₂
ReversibleY
Structure formula ImageStructure formula Image
Applications
Biological Information
Primary TargetDAAO
Primary Target IC<sub>50</sub>910 nM
Purity≥99% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code 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 InstructionsFollowing 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

Referencias bibliográficas

Visión general referencias
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.
Ficha técnica

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.

Revision08-March-2013 JSW
Synonyms5-methyl-1H-pyrazole-3-carboxylic acid, DAAO Inhibitor III
DescriptionA 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.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number402-61-9
Chemical formulaC₅H₆N₂O₂
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (50 mg/ml)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesSmith, 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.