420640 Ketohexokinase Inhibitor - Calbiochem

420640
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 Formula
      C₂₁H₂₆N₈S•2HCl

      Prix & Disponibilité

      Référence DisponibilitéConditionnement Qté Prix Quantité
      420640-10MG
      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 10 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
          OverviewAn orally bioavailable pyrimidinopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of human hepatic KHK activity (KHK-C isoform; IC50 = 12 nM in a transcreener ADP assay) and efficiently blocks fructose-1-phosphate secretion (IC50 ≤ 400 nM in HepG2 cells). Displays ~50-fold lower potency towards metabolic kinases, namely, ribokinase, hexokinase and adenosine kinase, and minimal binding affinities to diverse receptors and ion-channels, and excellent selectivity among a panel of 31-kinases including Akt1, AMPK, CaMKI/II, InsR, IRAK4, PKA and PKCθ (IC50 >> 10 µM). Shown to minimally affect the activities of human cytochrome p450 isozymes (1A2, 2C19, 2D6, 2C9 and 3A4), and exhibit high volume of distribution and high rate of clearance in rats.
          Catalogue Number420640
          Brand Family Calbiochem®
          SynonymsN⁸-(Cyclopropylmethyl)-N⁴-(2-(methylthio)phenyl)-2-(1-piperazinyl)-pyrimido[5,4-d]pyrimidine-4,8-diamine, KHK Inhibitor
          References
          ReferencesMaryanoff, B.E., et al. 2011. ACS Med. Chem. Lett. 2, 538.
          Product Information
          FormYellow solid
          Hill FormulaC₂₁H₂₆N₈S•2HCl
          Chemical formulaC₂₁H₂₆N₈S•2HCl
          Structure formula ImageStructure formula Image
          Quality LevelMQ100
          Applications
          Biological Information
          Purity≥97% 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 -20°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 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          Ketohexokinase Inhibitor - Calbiochem FDS

          Titre

          Fiche de données de sécurité des matériaux (FDS) 

          Ketohexokinase Inhibitor - Calbiochem Certificats d'analyse

          TitreNuméro de lot
          420640

          Références bibliographiques

          Aperçu de la référence bibliographique
          Maryanoff, B.E., et al. 2011. ACS Med. Chem. Lett. 2, 538.
          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.

          Revision22-February-2013 JSW
          SynonymsN⁸-(Cyclopropylmethyl)-N⁴-(2-(methylthio)phenyl)-2-(1-piperazinyl)-pyrimido[5,4-d]pyrimidine-4,8-diamine, KHK Inhibitor
          DescriptionAn orally bioavailable pyrimidinopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of human hepatic KHK activity (KHK-C isoform; IC50 = 12 nM in a transcreener ADP assay) and efficiently blocks fructose-1-phosphate secretion (IC50 ≤ 400 nM in HepG2 cells). Displays ~50-fold lower potency towards metabolic kinases, namely, ribokinase, hexokinase and adenosine kinase, and minimal binding affinities to diverse receptors and ion-channels, and excellent selectivity among a panel of 31-kinases including Akt1, AMPK, CaMKI/II, InsR, IRAK4, PKA and PKCθ (IC50 >> 10 µM). Shown to minimally affect the activities of human cytochrome p450 isozymes (1A2, 2C19, 2D6, 2C9 and 3A4), and exhibit high volume of distribution and high rate of clearance in rats.
          FormYellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₁H₂₆N₈S•2HCl
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (16.6 mg/ml)
          Storage -20°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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesMaryanoff, B.E., et al. 2011. ACS Med. Chem. Lett. 2, 538.