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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

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445874-5MG
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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
      Quality LevelMQ100
      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

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

      Title

      Safety Data Sheet (SDS) 

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