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

400093
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₂H₆ClF₃N₄O₃

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      400093-10MG
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          Glass bottle 10 mg
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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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          400093

          References

          Reference overview
          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.
          Data Sheet

          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.