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445874 Sigma-AldrichmGluR5 Antagonist, MTEP - CAS 329205-68-7 - Calbiochem

The mGluR5 Antagonist, MTEP, also referenced under CAS 329205-68-7, controls the biological activity of mGluR5. This small molecule/inhibitor is primarily used for Neuroscience applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
分析证书
参考
小册子
Data Sheet

同义词: 3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine

Primary Target: mGluR5

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
329205-68-7	C₁₁H₈N₂S

价格及供货情况

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Description
Overview	A 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; K_i = 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 Number	445874
Brand Family	Calbiochem®
Synonyms	3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine

References
References	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.

Product Information
CAS number	329205-68-7
ATP Competitive	N
Form	White to yellow solid
Hill Formula	C₁₁H₈N₂S
Chemical formula	C₁₁H₈N₂S
Reversible	N
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Primary Target	mGluR5
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 permeable	Y

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 Instructions	Following 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
产品目录编号	GTIN
445874-5MGCN	04055977204629

Documentation

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

职位
物料安全数据表 (MSDS)

mGluR5 Antagonist, MTEP - CAS 329205-68-7 - Calbiochem 分析证书

标题	批号
445874	输入批号

参考

参考信息概述
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.

小册子

标题
Pathways and Biomarkers of Glutamatergic Synapse Flyer

数据表

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.

Revision	19-June-2018 JSW
Synonyms	3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine
Description	A 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; K_i = 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).
Form	White to yellow solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	329205-68-7
Chemical formula	C₁₁H₈N₂S
Structure formula
Purity	≥98% by HPLC
Solubility	DMSO (5 mg/ml) or Methanol (1 mg/ml)
Storage	Protect from light +2°C to +8°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity	Standard Handling
References	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.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Neurochemicals > Antagonists > Glutamate Receptor Antagonists

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