MPEP Hydrochloride |
| Catalog No.GC16172 |
A potent, highly selective mGlu5a receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 219911-35-0
Sample solution is provided at 25 µL, 10mM.
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IC50: 36 nM
MPEP is a potent, selective and systemically active mGlu5 receptor antagonist.
Metabotropic glutamate (mGlu) receptors are a of G-protein-coupled receptor family linked to multiple second messengers and modulation of ion channel functions in the nervous system. Group I receptors (mGlu1 and -5) couple to phospholipase C and up or down regulate neuronal excitability (Gereau and Conn, 1995) whereas group II (mGlu2 and -3) and group III (mGlu4, -6, -7, and -8) receptors inhibit adenylyl cyclase and reduce synaptic transmission.
In vitro: In recombinant expressed cells human mGlu5a receptor, MPEP inhibited quisqualate-stimulated phosphoinositide hydrolysis completely with an IC50 value of 36 nM whereas with no agonist or antagonist activities at cells expressing the human mGlu1b receptor. MPEP did not show agonist or antagonist activity on human mGlu2, -3, -4a, -7b, and -8a receptors [1].
In vivo: In rat neonatal brain slices, MPEP inhibited DHPG-stimulated phosphoinositide hydrolysis with a potency and selectivity similar to that observed on human mGlu receptors. Moreover, in extracellular recordings in the hippocampus CA1 area of anesthetized rats, the microiontophoretic application of DHPG induced neuronal firing that was blocked when MPEP was administered [1].
Clinical trial: N/A
Reference:
[1] Gasparini F,Lingenhhl K,Stoehr N,Flor PJ,Heinrich M,Vranesic I,Biollaz M,Allgeier H,Heckendorn R,Urwyler S,Varney MA,Johnson EC,Hess SD,Rao SP,Sacaan AI,Santori EM,Velielebi G,Kuhn R. 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology.1999 Oct;38(10):1493-503.
| Cas No. | 219911-35-0 | SDF | |
| Chemical Name | 2-methyl-6-(2-phenylethynyl)pyridine;hydrochloride | ||
| Canonical SMILES | CC1=CC=CC(=N1)C#CC2=CC=CC=C2.Cl | ||
| Formula | C14H12ClN | M.Wt | 229.7 |
| Solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 5 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.3535 mL | 21.7675 mL | 43.535 mL |
| 5 mM | 0.8707 mL | 4.3535 mL | 8.707 mL |
| 10 mM | 0.4354 mL | 2.1768 mL | 4.3535 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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