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550601 Pyruvate Kinase Activator - CAS 1346113-84-5 - Calbiochem

The Pyruvate Kinase Activator controls the biological activity of Pyruvate Kinase. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

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Synonyme: PKM2 Activator I, N-(4-Chloro-3-fluorophenyl)-7-fluoro-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide

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550601
Preis & Verfügbarkeit

Übersicht

Replacement Information

Key Spec Table

Empirical Formula
C₁₅H₁₁ClF₂N₂O₃S

Preis & Verfügbarkeit

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550601-25MG
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      		 Glasflasche 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®
      SynonymsPKM2 Activator I, N-(4-Chloro-3-fluorophenyl)-7-fluoro-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
      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
      Global Trade Item Number
      Bestellnummer GTIN
      550601-25MG 04055977268867

      Documentation

      Pyruvate Kinase Activator - CAS 1346113-84-5 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Pyruvate Kinase Activator - CAS 1346113-84-5 - Calbiochem Analysenzertifikate

      TitelChargennummer
      550601

      Literatur

      Übersicht
      Walsh, M.J., et al. 2011. Bioorg. Med. Chem. Lett. 21, 6322.
      Datenblatt

      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
      SynonymsPKM2 Activator I, N-(4-Chloro-3-fluorophenyl)-7-fluoro-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
      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 Protect from light
      +2°C to +8°C
      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.