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Tocris/MPEP hydrochloride/1212/10/10 mg

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货号: 1212/10

品牌: Tocris

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Description: mGlu₅ antagonist and positive allosteric modulator at mGlu₄

Chemical Name: 2-Methyl-6-(phenylethynyl)pyridine hydrochloride

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent and highly selective non-competitive antagonist at the mGlu₅ receptor subtype (IC₅₀ = 36 nM) and a positive allosteric modulator at mGlu₄ receptors. Centrally active following systemic administration in vivo. Reverses mechanical hyperalgesia in the inflamed rat hind paw. Also available as part of the Group I mGlu Receptor Tocriset™.

Compound Libraries

MPEP hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	229.71
Formula	C₁₄H₁₁N.HCl
Storage	Desiccate at +4°C
Purity	≥99% (HPLC)
CAS Number	219911-35-0
PubChem ID	9794588
InChI Key	PKDHDJBNEKXCBI-UHFFFAOYSA-N
Smiles	Cl.CC1=CC=CC(=N1)C#CC1=CC=CC=C1

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	22.97	100
	ethanol	22.97	100
	water	1.15	5mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 229.71. 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	4.35 mL	21.77 mL	43.53 mL
5 mM	0.87 mL	4.35 mL	8.71 mL
10 mM	0.44 mL	2.18 mL	4.35 mL
50 mM	0.09 mL	0.44 mL	0.87 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Gasparini et al (1999) 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology 38 1493 PMID: 10530811

Mathiesen et al (2003) Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP. Br.J.Pharmacol. 138 1026 PMID: 12684257

Salt et al (1999) Antagonism of the mGlu5 agonist 2-chloro-5-hydroxyphenylglycine by the novel selective mGlu5 antagonist 6-methyl-2-(phenylethynyl)-pyridine (MPEP) in the thalamus. Br.J.Pharmacol. 127 1057 PMID: 10455248

Bowes et al (1999) Anti-hyperalgesic effects of the novel metabotropic glutamate receptor 5 antagonist, methylphenylethynylpyridine, in rat models of inflammatory pain. Br.J.Pharmacol. 126 250P PMID:

Keywords: MPEP hydrochloride, supplier, mGlu5, mGluR5, antagonists, positive, allosteric, modulators, mGlu4, mGluR4, PAM, Positive, Group, I, Receptors, Glutamate, Metabotropic, III, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, III, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience

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