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

251406
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Empirical Formula
C₅H₆N₂O₂

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251406-50MG
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      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
      Quality LevelMQ100
      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

      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.

      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.