MPEP

Name: MPEP
Brand: MedChemExpress
SKU: HY-14609A
Rating: 5.0 (4 reviews)

Cat. No.: HY-14609A Purity: 99.33%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

MPEP is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC₅₀ of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP has anxiolytic-or antidepressant-like effects. MPEP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

For research use only. We do not sell to patients.

MPEP Chemical Structure

CAS No. : 96206-92-7

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of MPEP:

MPEP Hydrochloride In-stock

4 Publications Citing Use of MCE MPEP

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View All Isoforms

mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

Biological Activity
Purity & Documentation
References
Customer Review

Description

MPEP is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC₅₀ of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP has anxiolytic-or antidepressant-like effects^[1]^[2]. MPEP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target^[1]

mGluR5

36 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.2 nM Compound: 1, MPEP	Activity at rat mGlu5 receptor expressed in CHO cells assessed as inhibition of quisqualate-stimulated calcium mobilization by FLIPR assay Activity at rat mGlu5 receptor expressed in CHO cells assessed as inhibition of quisqualate-stimulated calcium mobilization by FLIPR assay	[PMID: 17590335]
HEK293	IC₅₀	2.3 nM Compound: MPEP	Antagonist activity at human mGluR5 expressed in HEK293 cells assessed as inhibition of Ca2+ mobilization by FLIPR assay Antagonist activity at human mGluR5 expressed in HEK293 cells assessed as inhibition of Ca2+ mobilization by FLIPR assay	[PMID: 23357634]
HEK293	IC₅₀	32 nM Compound: MPEP	Negative allosteric modulator activity against human mGluR5 expressed in HEK293 cells assessed as inhibition of glutamate-induced inositol phosphate accumulation by IP-one HTRF assay Negative allosteric modulator activity against human mGluR5 expressed in HEK293 cells assessed as inhibition of glutamate-induced inositol phosphate accumulation by IP-one HTRF assay	[PMID: 26112438]
HEK293	IC₅₀	89 nM Compound: 10, MPEP	Negative allosteric modulator activity at rat mGlu5 receptor expressed in HEK293 cells assessed as effect on quisqualate-induced inositol phosphate accumulation incubated for 30 mins by florescence assay Negative allosteric modulator activity at rat mGlu5 receptor expressed in HEK293 cells assessed as effect on quisqualate-induced inositol phosphate accumulation incubated for 30 mins by florescence assay	10.1039/C4MD00208C
HEK293-A	IC₅₀	3.54 nM Compound: 1, MPEP	Antagonist activity at rat mGluR5 expressed in HEK293A cells assessed as glutamate-induced calcium flux preincubated for 140 sec before glutamate challenge by calcium fluorescence assay Antagonist activity at rat mGluR5 expressed in HEK293A cells assessed as glutamate-induced calcium flux preincubated for 140 sec before glutamate challenge by calcium fluorescence assay	[PMID: 19445453]
HEK293-A	IC₅₀	31 nM Compound: 1, MPEP	Inverse agonist activity at rat mGluR5 expressed in HEK293A cells coexpressing Gqalpha assessed as inhibition of quisqualic-induced D-myo-inositol 1 production by ELISA Inverse agonist activity at rat mGluR5 expressed in HEK293A cells coexpressing Gqalpha assessed as inhibition of quisqualic-induced D-myo-inositol 1 production by ELISA	[PMID: 22924094]
HEK-293T	IC₅₀	3.54 nM Compound: 1, MPEP	Antagonist activity at rat mGluR5 expressed in HEK293T cells assessed as inhibition of glutamate-induced calcium flux by calcium fluorescence assay Antagonist activity at rat mGluR5 expressed in HEK293T cells assessed as inhibition of glutamate-induced calcium flux by calcium fluorescence assay	[PMID: 21295978]

In Vitro

MPEP does not show agonist or antagonist activity at 100 mM on human mGlu2, -3, -4a, -7b, and -8a receptors nor at 10 μM on the human mGlu6 receptor^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

MPEP (1-30 mg/kg) induces anxiolytic-like effects in the conflict drinking test and the elevated plus-maze test in rats as well as in the four-plate test in mice^[2].
MPEP (1-20 mg/kg) does shorten the immobility time in a tail suspension test in mice, however it is inactive in the behavioural despair test in rats^[2].
MPEP (30 mg/kg i.p.) slightly but significantly increases (by 39%) the number of punished crossings in the four-plate test, lower doses of the compound (3 and 10 mg/kg) does not affect the number of punished crossings in that test (F (3,36)=3.240, P<0.05)^[2].
MPEP (1, 10 and 20 mg/kg) significantly (by 55% after the highest dose), (F(3,28)=15.47, P<0.001) decreases the immobility time of mice in the tail suspension test. Its efficacy is similar to that of imipramine (20 mg/kg), used as the positive standard^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Wistar rats (200 ± 250 g)^[2].
Dosage:	IP or PO.
Administration:	0.3, 1 and 10 mg/kg, i.p. (Conflict drinking test).
Result:	At a dose of 0.3 mg/kg was not ffective, at doses of 1 and 10 mg/kg i.p. significantly (F (3,30)=11.193, P<0.001), increased the number of shocks (by 330 and 507%, respectively) accepted during the experimental session in the Vogel test.

Animal Model:	Male Wistar rats (200 ± 250 g)^[2].
Dosage:	IP or PO.
Administration:	1, 3 and 10 mg/kg, i.p. or 10 and 30 mg/kg, p.o.(Elevated plus-maze test).
Result:	Administered at a dose of 1 mg kg71 i.p. did not change the entries into and time spent in the open arms. At doses of 3 and 10 mg/kg i.p. significantly (F (3,24)=22.978, P<0.001) dose-dependently increased the time spent in the open arms (up to 45 and 74%, respectively), and the percentage of entries into the open arms (up to 48 and 68%, respectively, F(3,24)=5.678, P<.01). At doses of 3 and 10 mg/kg i.p. significantly increased (by 64%) the total number of entries and reduced (by about 25%) the total time spent (data not shown) in the arms (either type). At the dose of 30 mg/kg (po, but not 10 mg/kg) significantly (up to 64%, F (2,16)=14.249, P<0.001) increased the percentage of the time spent in the open arms and the percentage of entries into the open arms (up to 63%, F (2,16)=7.295, P<0.01). MPEP given p.o. in both doses used did not change the total number of entries nor the total time spent in the arms (either type).

Molecular Weight

193.24

Formula

C₁₄H₁₁N

CAS No.

96206-92-7

Appearance

Solid

Color

Yellow to brown

SMILES

CC1=NC(C#CC2=CC=CC=C2)=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (517.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	5.1749 mL	25.8746 mL	51.7491 mL
5 mM	1.0350 mL	5.1749 mL	10.3498 mL
10 mM	0.5175 mL	2.5875 mL	5.1749 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (12.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (12.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.33%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (247 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

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

[2]. E Tatarczyńska, et al. 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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	5.1749 mL	25.8746 mL	51.7491 mL	129.3728 mL
	5 mM	1.0350 mL	5.1749 mL	10.3498 mL	25.8746 mL
	10 mM	0.5175 mL	2.5875 mL	5.1749 mL	12.9373 mL
	15 mM	0.3450 mL	1.7250 mL	3.4499 mL	8.6249 mL
	20 mM	0.2587 mL	1.2937 mL	2.5875 mL	6.4686 mL
	25 mM	0.2070 mL	1.0350 mL	2.0700 mL	5.1749 mL
	30 mM	0.1725 mL	0.8625 mL	1.7250 mL	4.3124 mL
	40 mM	0.1294 mL	0.6469 mL	1.2937 mL	3.2343 mL
	50 mM	0.1035 mL	0.5175 mL	1.0350 mL	2.5875 mL
	60 mM	0.0862 mL	0.4312 mL	0.8625 mL	2.1562 mL
	80 mM	0.0647 mL	0.3234 mL	0.6469 mL	1.6172 mL
	100 mM	0.0517 mL	0.2587 mL	0.5175 mL	1.2937 mL

MPEP Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MPEP96206-92-7mGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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Customer Review

Other Forms of MPEP:

MPEP Related Antibodies

4 Publications Citing Use of MCE MPEP

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•Related Screening Libraries:

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View All mGluR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

MPEP Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

MPEP Related Classifications

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