531145 mGlu7 Antagonist, XAP044 - Calbiochem

531145
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₅H₉IO₄ 196928-50-4

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      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.31145.0001
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          Glass bottle 10 mg
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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
          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

          Documentation

          mGlu7 Antagonist, XAP044 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Gee, C.E., et al. 2014. J. Biol. Chem. 289, 10975.
          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-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 +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
          ReferencesGee, C.E., et al. 2014. J. Biol. Chem. 289, 10975.