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531145 mGlu7 Antagonist, XAP044 - Calbiochem

A blood-brain barrier permeable, potent, selective, and reversible antagonist of mGlu7 receptor (IC₅₀ = 3.5 and 2.8 µM for mGlu7a and mGlu7b in CHO cells).

mGlu7 Antagonist, XAP044 - Calbiochem : FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: 7-Hydroxy-3-(4-iodophenoxy)-4H-chromen-4-one, 7-Hydroxy-3-(4-iodophenoxy)-chromen-4-one, Metabotropic Glutamate Receptor Subtype 7 Antagonist, XAP-044

Primary Target: mGlu7R
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531145
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CAS #Empirical Formula
196928-50-4C₁₅H₉IO₄

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      Description
      OverviewA blood-brain barrier permeable and bioavailable chromenone compound that acts as a potent, selective, and reversible antagonist of mGlu7 receptor (IC50 = 3.5 and 2.8 µM for mGlu7a and mGlu7b in CHO cells). Docks within the Venus flytrap domain (VFTD) close to the binding site of L-glutamate and functions as an orthosteric-like antagonist. Reduces DL-2-amino-4-phosphonobutyric acid (DL-AP4)-induced activation of human mGlu7b receptor (IC50 = 2.8 µM), but does not affect DL-AP4-induced activation of [35S]GTPγS binding by mGlu4 and mGlu6. Shown to diminish [35S]GTPγS binding by the human mGlu7/6 chimeric receptor harboring mGlu7 VFTD (IC50 = 2.5 µM). Displays weak binding affinity towards mGlu5 and mGlu8 receptors (IC50 > 20 and 33 µM, respectively) and has no effect on GABA-induced activation of [35S]GTPγS binding by GABA-B receptors. Displays antidepressant and anxiolytic-like properties and selectively blocks long-term potentiation (LTP) in the lateral amygdala of wild type (IC50 = 88 nM), but not of mGlu7- deficient mice.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number531145
      Brand Family Calbiochem®
      Synonyms7-Hydroxy-3-(4-iodophenoxy)-4H-chromen-4-one, 7-Hydroxy-3-(4-iodophenoxy)-chromen-4-one, Metabotropic Glutamate Receptor Subtype 7 Antagonist, XAP-044
      References
      ReferencesGee, C.E., et al. 2014. J. Biol. Chem. 289, 10975.
      Product Information
      CAS number196928-50-4
      FormPale yellow powder
      Hill FormulaC₁₅H₉IO₄
      Chemical formulaC₁₅H₉IO₄
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetmGlu7R
      Primary Target IC<sub>50</sub>3.5 and 2.8 µ
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      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
      Référence GTIN
      5.31145.0001 04055977242645

      Documentation

      mGlu7 Antagonist, XAP044 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Gee, C.E., et al. 2014. J. Biol. Chem. 289, 10975.
      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-July-2014 JSW
      Synonyms7-Hydroxy-3-(4-iodophenoxy)-4H-chromen-4-one, 7-Hydroxy-3-(4-iodophenoxy)-chromen-4-one, Metabotropic Glutamate Receptor Subtype 7 Antagonist, XAP-044
      DescriptionA blood-brain barrier permeable and bioavailable chromenone compound that acts as a potent, selective, and reversible antagonist of mGlu7 receptor (IC50 = 3.5 and 2.8 µM for mGlu7a and mGlu7b in CHO cells). Docks within the Venus flytrap domain (VFTD) close to the binding site of L-glutamate and functions as an orthosteric-like antagonist. Reduces DL-2-amino-4-phosphonobutyric acid (DL-AP4)-induced activation of human mGlu7b receptor (IC50 = 2.8 µM), but does not affect DL-AP4-induced activation of [35S]GTPγS binding by mGlu4 and mGlu6. Shown to diminish [35S]GTPγS binding by the human mGlu7/6 chimeric receptor harboring mGlu7 VFTD (IC50 = 2.5 µM). Displays weak binding affinity towards mGlu5 and mGlu8 receptors (IC50 > 20 and 33 µM, respectively) and has no effect on GABA-induced activation of [35S]GTPγS binding by GABA-B receptors. Displays antidepressant and anxiolytic-like properties and selectively blocks long-term potentiation (LTP) in the lateral amygdala of wild type (IC50 = 88 nM), but not of mGlu7- deficient mice.
      FormPale yellow powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number196928-50-4
      Chemical formulaC₁₅H₉IO₄
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml)
      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
      ReferencesGee, C.E., et al. 2014. J. Biol. Chem. 289, 10975.