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Tocris/MTEP hydrochloride/2921/10/10 mg

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货号: 2921/10

品牌: Tocris

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Description: Potent, selective mGlu₅ antagonist

Chemical Name: 3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine hydrochloride

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent, selective and non-competitive mGlu₅ antagonist (IC₅₀ = 5 nM in Ca²⁺-flux assay; K_i= 16 nM). Displays anxiolytic activity in vivo and is orally active.

Licensing Information

Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans)

Technical Data

M. Wt	236.72
Formula	C₁₁H₈N₂S.HCl
Storage	Store at -20°C
Purity	≥99% (HPLC)
CAS Number	1186195-60-7
PubChem ID	45073467
InChI Key	YCIOJDKGCWAHLR-UHFFFAOYSA-N
Smiles	CC1=NC(C#CC2=CN=CC=C2)=CS1.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	23.67	100
	water	23.67	100

Preparing Stock Solutions

The following data is based on the product molecular weight 236.72. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	4.22 mL	21.12 mL	42.24 mL
5 mM	0.84 mL	4.22 mL	8.45 mL
10 mM	0.42 mL	2.11 mL	4.22 mL
50 mM	0.08 mL	0.42 mL	0.84 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Bradbury et al (2005) Metabotropic glutamate receptor mGlu5 is a mediator of appetite and energy balance in rats and mice. J.Pharmacol.Exp.Ther. 313 395 PMID: 15590770

Roppe et al (2004) 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. Bioorg.Med.Chem.Lett. 14 3993 PMID: 15225713

Klodzinska et al (2004) Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABA_A signaling. Neuropharmacology 47 342 PMID: 15275823

Cosford et al (2003) 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]- pyridine: A potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. J.Med.Chem. 46 204 PMID: 12519057

Brodkin et al (2002) Reduced stress-induced hyperthermia in mGluR5 knockout mice. Eur.J.Neurosci. 16 2241 PMID: 12473093

Keywords: MTEP hydrochloride, supplier, Potent, selective, mGlu5, mGluR5, antagonists, mGlur, Group, I, Receptors, Glutamate, Metabotropic, merck, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience

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