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400093 HIF-PHD Inhibitor II, JNJ-42041935 - Calbiochem

400093
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Tableau de caractéristiques principal

Empirical Formula
C₁₂H₆ClF₃N₄O₃

Prix & Disponibilité

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400093-10MG
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      Description
      OverviewA cell-permeable benzimidazolopyrazole compound that acts as an active-site binding, iron insensitive, 2-oxoglutarate competitive, reversible and potent inhibitor of PHD1, 2 and 3 isozymes (pKi = 7.91, 7.29 and 7.65, respectively). Displays >100-fold selectivity over FIH (factor inhibiting hydroxylase; pIC50 ~ 4) and minimal affinity towards a panel of receptors, enzymes and kinases. Shown to elevate HIF-1α levels in Hep3B cells and stimulate erythropoietin secretion in mice, and reverse inflammation-induced anemia in rats (100 µM/kg). Shown to inhibit malate dehydrogenase 2 (MDH2) activity and suppress mitochondrial respiration.
      Catalogue Number400093
      Brand Family Calbiochem®
      Synonyms1-(5-Chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid, HIF Prolyl Hydroxylase Inhibitor II
      References
      ReferencesLee, K., et al., 2013. Angew. Chem. Int. Ed. 52, In press.
      Barrett, T.D., et al. 2011. Mol. Pharmacol. 79, 910.
      Rosen, M.D., et al. 2010. ACS Med. Chem. Lett. 1, 526.
      Product Information
      FormWhite solid
      Hill FormulaC₁₂H₆ClF₃N₄O₃
      Chemical formulaC₁₂H₆ClF₃N₄O₃
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      HIF-PHD Inhibitor II, JNJ-42041935 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      HIF-PHD Inhibitor II, JNJ-42041935 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      400093

      Références bibliographiques

      Aperçu de la référence bibliographique
      Lee, K., et al., 2013. Angew. Chem. Int. Ed. 52, In press.
      Barrett, T.D., et al. 2011. Mol. Pharmacol. 79, 910.
      Rosen, M.D., et al. 2010. ACS Med. Chem. Lett. 1, 526.
      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.

      Revision31-August-2012 JSW
      Synonyms1-(5-Chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid, HIF Prolyl Hydroxylase Inhibitor II
      DescriptionA cell-permeable benzimidazolopyrazole compound that acts as an active-site binding, iron insensitive, 2-oxoglutarate competitive, reversible and potent inhibitor of PHD1, 2 and 3 isozymes (pKi = 7.91, 7.29 and 7.65, respectively). Displays >100-fold selectivity over FIH (factor inhibiting hydroxylase; pIC50 ~ 4) and minimal affinity towards a panel of receptors, enzymes and kinases. Shown to elevate HIF-1α levels in Hep3B cells and stimulate erythropoietin secretion in mice, and reverse inflammation-induced anemia in rats (100 µM/kg).
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₂H₆ClF₃N₄O₃
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (100 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 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesLee, K., et al., 2013. Angew. Chem. Int. Ed. 52, In press.
      Barrett, T.D., et al. 2011. Mol. Pharmacol. 79, 910.
      Rosen, M.D., et al. 2010. ACS Med. Chem. Lett. 1, 526.