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

251406
Le prix n'a pas pu être récupéré
La quantité minimale doit être un multiple de
À la validation de la commande Plus d'informations
Vous avez sauvegardé ()
 
Demander le prix
Disponibilité limitéeDisponibilité limitée
En stock 
Interrompu(e)
Disponible en quantités limitées
Disponibilité à confirmer
    Pour le restant : Nous vous tiendrons informé
      Pour le restant : Nous vous tiendrons informé
      Nous vous tiendrons informé
      Contacter le Service Clients
      Contact Customer Service
      Voir les Prix & la Disponibilité

      Aperçu

      Replacement Information

      Tableau de caractéristiques principal

      Empirical FormulaCAS #
      C₅H₆N₂O₂ 402-61-9

      Prix & Disponibilité

      Référence DisponibilitéConditionnement Qté Prix Quantité
      251406-50MG
      Récupération des données relatives à la disponibilité...
      Disponibilité limitéeDisponibilité limitée
      En stock 
      Interrompu(e)
      Disponible en quantités limitées
      Disponibilité à confirmer
        Pour le restant : Nous vous tiendrons informé
          Pour le restant : Nous vous tiendrons informé
          Nous vous tiendrons informé
          Contacter le Service Clients
          Contact Customer Service

          Flacon en verre 50 mg
          Prix en cours de récupération
          Le prix n'a pas pu être récupéré
          La quantité minimale doit être un multiple de
          À la validation de la commande Plus d'informations
          Vous avez sauvegardé ()
           
          Demander le prix
          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.