MPEP hydrochloride

Alias: 2-methyl-6-(phenylethynyl)-pyridine;MPEP; MPEP HCl; MPEP hydrochloride

Cat No.:V3421 Purity: ≥98%

COA Product Data Instructions for use SDS

MPEP hydrochloride is a highly potent, selective, and non-competitive antagonist of mGlu5 receptor with IC50 of 36 nM, it exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors.

MPEP hydrochloride Chemical Structure CAS No.: 219911-35-0
Product category: mGluR

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of MPEP hydrochloride:

MPEP

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

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Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Biological Data

Product Description

MPEP hydrochloride is a highly potent, selective, and non-competitive antagonist of mGlu5 receptor with IC50 of 36 nM, it exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors. In mice lacking Fmr1, MPEP improves maze learning and PSD-95 deficiencies. MPEP does not cause harm to the adult retrosplenial cortex, unlike the NMDA antagonist MK-801, where it is unable to induce heat shock protein 70 (Hsp70). Additionally, as demonstrated by caspase 3 expression, MPEP does not induce apoptosis in cortical areas during perinatal stages to the same degree as MK-801. The anxiolytic and antidepressant effects of MPEP have been linked to new cellular targets by these data, which also show that MPEP does not have the cortical neurotoxicity linked to psychotomimetic side effects that is present in MK-801. The medication MPEP may be used as an antidepressant or anxiolytic.

Biological Activity I Assay Protocols (From Reference)

Targets

mGluR5 ( IC50 = 36 nM )

ln Vitro

In vitro activity: MPEP exhibits neither agonist nor antagonist activity at 100 mM on human mGlu2, -3, -4a, -7b, and -8a receptors, as well as at 10 μM on the human mGlu6 receptor[1].

ln Vivo

MPEP (1-30 mg/kg) causes anxiolytic-like effects in the conflict drinking test, the elevated plus-maze test, and the four-plate test in mice[2].
MPEP (1–20 mg/kg) does reduce the immobility period in mice; however, in a behavioral despair test, it has no effect in rats in a tail suspension test[2].
MPEP (30 mg/kg i.p.) marginally but significantly raises the number of crossings that result in a penalty (by 39%); lower concentrations of the compound (3 and 10 mg/kg) have no effect on this number (F (3,36)=3.240, P<0.05) in the four-plate test[2].
MPEP (1, 10 and 20 mg/kg) significantly reduces the immobility time of mice (by 55% after the highest dose; F(3,28)=15.47, P<0.001) in the tail suspension test. Its effectiveness is comparable to that of imipramine (20 mg/kg), which is the gold standard[2].

Enzyme Assay

MPEP has an IC50 of 36 nM and is a very strong, selective, and non-competitive mGlu5 receptor antagonist. It shows no discernible activity at mGlu1b/2/3/4a/7b/8a/6 receptors.

Cell Assay

In slices of rat neonatal hippocampus, striatum, and cortex but not cerebellum, MPEP inhibits DHPG-stimulated PI hydrolysis with IC50 of 8.0 nM, 20.5 nM, and 17.9 nM, respectively. MPEP activates the orthosteric agonist L-AP4, which is necessary for MPEP to have any effect. MPEP positively modulates hmGluR4 in a recombinant expression system.

Animal Protocol

Suspended in a 1% aqueous solution of Tween 80; 30 mg/kg; i.p. or p.o. administration

Male Wistar rats, male Albino Swiss mice, or male C57BL/6J mice subjected to various tests

References

[1]. 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a Potent, Selective and Systemically Active mGlu5 Receptor Antagonist. Neuropharmacology. 1999 Oct;38(10):1493-503.

[2]. Potential anxiolytic- and antidepressant-like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist. Br J Pharmacol. 2001 Apr;132(7):1423-30.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C14H12CLN
Molecular Weight	229.70478
Exact Mass	229.07
Elemental Analysis	C, 73.20; H, 5.27; Cl, 15.43; N, 6.10
CAS #	219911-35-0
Related CAS #	MPEP; 96206-92-7
Appearance	Yellow solid powder
SMILES	CC1=NC(=CC=C1)C#CC2=CC=CC=C2.Cl
InChi Key	PKDHDJBNEKXCBI-UHFFFAOYSA-N
InChi Code	InChI=1S/C14H11N.ClH/c1-12-6-5-9-14(15-12)11-10-13-7-3-2-4-8-13;/h2-9H,1H3;1H
Chemical Name	2-methyl-6-(2-phenylethynyl)pyridine;hydrochloride
Synonyms	2-methyl-6-(phenylethynyl)-pyridine;MPEP; MPEP HCl; MPEP hydrochloride
HS Tariff Code	2934.99.9001
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: >10 mM

Water:

Ethanol:

Solubility (In Vivo)

Solubility in Formulation 1: 100 mg/mL (435.35 mM) in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: 2% DMSO+30% PEG 300+5% Tween 80: 10 mg/mL

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	4.3535 mL	21.7675 mL	43.5350 mL
	5 mM	0.8707 mL	4.3535 mL	8.7070 mL
	10 mM	0.4354 mL	2.1768 mL	4.3535 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
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See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
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The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
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The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Biological Data

Effects of MPEP and diazepam in the four-plate test in mice. Br J Pharmacol. 2001 Apr;132(7):1423-30.Br J Pharmacol.2001 Apr;132(7):1423-30.
The effects of MPEP and imipramine on the total duration of immobility in the tail suspension test in mice. Br J Pharmacol. 2001 Apr;132(7):1423-30.Br J Pharmacol.2001 Apr;132(7):1423-30.
The effects of MPEP and imipramine on the total duration of immobility in the forced swimming test in rats.Br J Pharmacol.2001 Apr;132(7):1423-30.
Induction of c-Fos and Hsp70 expression in cortical areas associated with psychosis after treatment with MK-801 and MPEP in adult rodents.Neuropharmacology.2012Apr;62(5-6):2034-9.
Dose-dependent c-Fos induction by MPEP in stress-related brain regions.Neuropharmacology.2012Apr;62(5-6):2034-9.

MPEP hydrochloride

Comparison of the apoptosis induced by MPEP vs. MK-801 in the retrosplenial cortex at P7. Compared to vehicle (A) and MPEP (100mg/kg), MK-801 (0,5mg/kg) induces a widespread apoptosis in the cortex, including the retrosplenial cortex (C), also visible in panel D.Neuropharmacology.2012Apr;62(5-6):2034-9.