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550601 Pyruvate Kinase Activator - Calbiochem

550601
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₅H₁₁ClF₂N₂O₃S

Pricing & Availability

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550601-25MGCN
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      玻璃瓶 25 mg
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      Description
      OverviewA cell-permeable and biologically stable (t1/2 = 277.2 and 117.5 min., respectively, in human and mouse liver microsome preparation) tetrahydroquinoline-sulfonamide that enhances the donor PEP, but not the acceptor ADP, substrate affinity toward pyruvate kinase isoform PKM2 (Km = 0.4 vs. 1.9 mM with or without 10 µM activator) and acts as a potent PKM2-selective activator (AC50 = 90 nM using rhPKM2; ACmax = 88%), displaying much reduced activity toward PKL (≤25% at 57 µM) and no effect toward PKM1 or PKR.
      Catalogue Number550601
      Brand Family Calbiochem®
      SynonymsN-(4-Chloro-3-fluorophenyl)-7-fluoro-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide, PKM2 Activator I
      References
      ReferencesWalsh, M.J., et al. 2011. Bioorg. Med. Chem. Lett. 21, 6322.
      Product Information
      FormWhite powder
      Hill FormulaC₁₅H₁₁ClF₂N₂O₃S
      Chemical formulaC₁₅H₁₁ClF₂N₂O₃S
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% 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 Ambient Temperature Only
      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

      Pyruvate Kinase Activator - Calbiochem MSDS

      Title

      Safety Data Sheet (SDS) 

      Pyruvate Kinase Activator - Calbiochem Certificates of Analysis

      TitleLot Number
      550601

      References

      Reference overview
      Walsh, M.J., et al. 2011. Bioorg. Med. Chem. Lett. 21, 6322.
      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.

      Revision02-October-2012 JSW
      SynonymsN-(4-Chloro-3-fluorophenyl)-7-fluoro-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide, PKM2 Activator I
      DescriptionA cell-permeable (Papp x 106 = 9.38 and 7.91 cm/s, respectively, for "A-B" and "B-A" in Caco-2 permeability assay) and biologically stable (t1/2 = 277.2 and 117.5 min., respectively, using human and mouse liver microsome preparation) tetrahydroquinoline-sulfonamide that enhances the donor PEP (phosphoenolpyruvate), but not the acceptor ADP, substrate affinity toward PK (pyruvate kinase) isoform PKM2 (Km = 0.4 vs. 1.9 mM with or without 10 µM activator) and acts as a potent PKM2-selective activator (AC50 = 90 nM using rhPKM2; ACmax = 88%), displaying much reduced activity toward PKL (≤25% at 57 µM) and no effect toward PKM1 or PKR.
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₅H₁₁ClF₂N₂O₃S
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml; clear, colorless solution)
      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
      ReferencesWalsh, M.J., et al. 2011. Bioorg. Med. Chem. Lett. 21, 6322.