445874 mGluR5 Antagonist, MTEP - CAS 329205-68-7 - Calbiochem

445874
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₁H₈N₂S 329205-68-7

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      445874-5MG
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          Plastic ampoule 5 mg
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          Description
          OverviewA brain-permeable (thiazole-pyridine)alkyne compound that acts as a potent, selective and non-competitive mGluR5 (metabotropic glutamate receptor subtype-5) antagonist (IC50 = 5 nM in Ca2+-flux assay; Ki = 16 nM) with in vivo anxiolytic activity in a rodent model (ED50 = 1 mg/kg, ip and 7 mg/kg, po). Devoid of any side effects seen with MPEP and benzodiazepines. Reported to weakly affect the activities of other enzymes and receptors tested (IC50 = 30 µM for MAO-A, > 100 µM for mGlu1R, 2R & 7R, and > 300 µM for NR2BR).
          Catalogue Number445874
          Brand Family Calbiochem®
          Synonyms3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine
          References
          ReferencesBradbury, M.J., et al. 2005. J. Pharmacol. Exp. Ther. 313, 395.
          Busse, C.S., et al. 2004. Neuropsychopharmacology 29, 1971.
          Roppe, J.R., et al. 2004. Bioorg. Med. Chem. Lett. 14, 3993.
          Klodzinska, A., et al. 2004. Neuropharmacology 47, 342.
          Cosford, N.D.P., et al. 2003. J. Med. Chem. 46, 204.
          Brodkin, J., et al. 2002. Eur. J. Neurosci. 16, 2241.
          Product Information
          CAS number329205-68-7
          ATP CompetitiveN
          FormWhite to yellow solid
          Hill FormulaC₁₁H₈N₂S
          Chemical formulaC₁₁H₈N₂S
          ReversibleN
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetmGluR5
          Primary Target IC<sub>50</sub>5 nM in Ca2+-flux assay
          Primary Target K<sub>i</sub>16 nM for mGluR5 (metabotropic glutamate receptor subtype-5)
          Purity≥98% 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 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
          445874

          References

          Reference overview
          Bradbury, M.J., et al. 2005. J. Pharmacol. Exp. Ther. 313, 395.
          Busse, C.S., et al. 2004. Neuropsychopharmacology 29, 1971.
          Roppe, J.R., et al. 2004. Bioorg. Med. Chem. Lett. 14, 3993.
          Klodzinska, A., et al. 2004. Neuropharmacology 47, 342.
          Cosford, N.D.P., et al. 2003. J. Med. Chem. 46, 204.
          Brodkin, J., et al. 2002. Eur. J. Neurosci. 16, 2241.

          Brochure

          Title
          Calbiochem Biologics 32.2
          Pathways and Biomarkers of Glutamatergic Synapse Flyer (EMD)
          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.

          Revision19-June-2018 JSW
          Synonyms3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine
          DescriptionA brain-permeable (thiazole-pyridine)alkyne compound that acts as a potent, selective and non-competitive mGluR5 (metabotropic glutamate receptor subtype-5) antagonist (IC50 = 5 nM in Ca2+-flux assay; Ki = 16 nM) with in vivo anxiolytic activity in a rodent model (ED50 = 1 mg/kg, ip and 7 mg/kg, po). Devoid of any side effects seen with MPEP and benzodiazepines. Reported to weakly affect the activities of other enzymes and receptors tested (IC50 = 30 µM for MAO-A, >100 µM for mGlu1R, 2R & 7R, and >300 µM for NR2BR).
          FormWhite to yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number329205-68-7
          Chemical formulaC₁₁H₈N₂S
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (5 mg/ml) or Methanol (1 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
          ReferencesBradbury, M.J., et al. 2005. J. Pharmacol. Exp. Ther. 313, 395.
          Busse, C.S., et al. 2004. Neuropsychopharmacology 29, 1971.
          Roppe, J.R., et al. 2004. Bioorg. Med. Chem. Lett. 14, 3993.
          Klodzinska, A., et al. 2004. Neuropharmacology 47, 342.
          Cosford, N.D.P., et al. 2003. J. Med. Chem. 46, 204.
          Brodkin, J., et al. 2002. Eur. J. Neurosci. 16, 2241.