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

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Synonymes: 5-methyl-1H-pyrazole-3-carboxylic acid, DAAO Inhibitor III

Primary Target: DAAO
251406
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      Tableau de caractéristiques principal

      Empirical FormulaCAS #
      C₅H₆N₂O₂ 402-61-9

      Prix & Disponibilité

      Référence DisponibilitéConditionnement Qté Prix Quantité
      251406-50MG
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          		 Flacon en verre 50 mg
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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.