1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. MTEP

MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research. MTEP 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.

MTEP

MTEP Chemical Structure

CAS No. : 329205-68-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
Solid
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of MTEP:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research[1][2][3][4]. MTEP 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

mGluR5

5 nM (IC50)

mGluR5

16 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.462 μM
Compound: 4
Antagonist activity against mGluR5 expressed in CHO cells assessed as inhibition of agonist-induced phosphoinositide hydrolysis
Antagonist activity against mGluR5 expressed in CHO cells assessed as inhibition of agonist-induced phosphoinositide hydrolysis
[PMID: 16678408]
CHO IC50
462 nM
Compound: 22
Activity in agonist-induced phosphoinositide hydrolysis in CHO cells expressing mGluR5a
Activity in agonist-induced phosphoinositide hydrolysis in CHO cells expressing mGluR5a
[PMID: 16451073]
HEK293 IC50
12 nM
Compound: MTEP
Negative allosteric modulation of human mGluR5 expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
Negative allosteric modulation of human mGluR5 expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
[PMID: 23434029]
HEK293 IC50
5 nM
Compound: MTEP
Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization
Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization
[PMID: 21546249]
HEK293-A IC50
110 nM
Compound: 2, MTEP
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]
HEK293-A IC50
13.6 nM
Compound: 2
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]
In Vitro

MTEP shows highly selective for mGluR5 over mGluR1, has no effect on other mGluR subtypes, and has fewer off-target effects than MPEP (HY-14609A)[1].

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

In Vivo

MTEP (0-5 mg/kg, i.p., once) inhibits the catalepsy induced by Haloperidol (HY-14538) (0.5 mg/kg/2 ml i.p.)[2].
MTEP (0.3-3 mg/kg, intraperitoneal injection, once) induces antidepressant-like effects in male C57BL/6J mice[3].

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

Animal Model: Male Wistar rats (215-315 g, 5-9/group)[2]
Dosage: 1, 3 and 5 mg/kg
Administration: IP, once, injected 60 min after Haloperidol (HY-14538) (0.5 mg/kg/2 ml i.p.)
Result: Inhibited the catalepsy induced by Haloperidol (HY-14538).
Animal Model: Male C57BL/6J mice (23-25 g)[3]
Dosage: 0.3, 1 and 3 mg/kg
Administration: IP, 1 h before the test
Result: Significantly decreased the immobility time of mice in the tail suspension test (TST) by 24%, 41% and 48%, respectively. The efficacy of MTEP used at doses of 1 and 3 mg/kg was not significantly different from that of Imipramine (HY-B1490A) (20 mg/kg, ip), used as a positive standard.
Molecular Weight

200.26

Formula

C11H8N2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=NC(C#CC2=CC=CN=C2)=CS1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (499.35 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 4.9935 mL 24.9675 mL 49.9351 mL
5 mM 0.9987 mL 4.9935 mL 9.9870 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.9935 mL 24.9675 mL 49.9351 mL 124.8377 mL
5 mM 0.9987 mL 4.9935 mL 9.9870 mL 24.9675 mL
10 mM 0.4994 mL 2.4968 mL 4.9935 mL 12.4838 mL
15 mM 0.3329 mL 1.6645 mL 3.3290 mL 8.3225 mL
20 mM 0.2497 mL 1.2484 mL 2.4968 mL 6.2419 mL
25 mM 0.1997 mL 0.9987 mL 1.9974 mL 4.9935 mL
30 mM 0.1665 mL 0.8323 mL 1.6645 mL 4.1613 mL
40 mM 0.1248 mL 0.6242 mL 1.2484 mL 3.1209 mL
50 mM 0.0999 mL 0.4994 mL 0.9987 mL 2.4968 mL
60 mM 0.0832 mL 0.4161 mL 0.8323 mL 2.0806 mL
80 mM 0.0624 mL 0.3121 mL 0.6242 mL 1.5605 mL
100 mM 0.0499 mL 0.2497 mL 0.4994 mL 1.2484 mL
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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.

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MTEP
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