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

445874
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
329205-68-7C₁₁H₈N₂S

Products

Catalogue NumberPackaging Qty/Pack
445874-5MG Plastic ampoule 5 mg
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.

Brochure

Title
Pathways and Biomarkers of Glutamatergic Synapse Flyer
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.