Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
SKU | Size | Availability | Price | Qty |
---|---|---|---|---|
M127959-10mg | 10mg | In stock | $86.90 | |
M127959-50mg | 50mg | In stock | $216.90 | |
M127959-250mg | 250mg | In stock | $692.90 | |
M127959-1g | 1g | In stock | $2,494.90 |
Potent, selective mGlu 5 antagonist
Synonyms | NCGC00025044-01 | NCGC00025044-02 | Pyridine, 6-methyl-2-(phenylethynyl)- | 2-Picoline, 6-phenylethynyl- | NCGC00015682-04 | SMR004702989 | MLS006011229 | 7VC0YVI27Y | 2-methyl-6-(2-phenylethynyl)pyridine | Lopac0_000738 | SCHEMBL103061 | AM81262 | Tocris |
---|---|
Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | MPEP is a 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 hyperalge |
Storage Temp | Store at -20°C,Argon charged |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | ALLOSTERIC MODULATOR |
Mechanism of action | Allosteric modulator of mGlu 4 receptor;Allosteric modulator of mGlu 5 receptor |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | MPEP is a selective mGlu5 receptor antagonist with IC50 of 36 nM, exhibits no appreciable activity at mGlu1b/2/3/4a/7b/8a/6 receptors. |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
---|
Pubchem Sid | 488194193 |
---|---|
Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/488194193 |
IUPAC Name | 2-methyl-6-(2-phenylethynyl)pyridine |
INCHI | InChI=1S/C14H11N/c1-12-6-5-9-14(15-12)11-10-13-7-3-2-4-8-13/h2-9H,1H3 |
InChi Key | NEWKHUASLBMWRE-UHFFFAOYSA-N |
Canonical SMILES | CC1=NC(=CC=C1)C#CC2=CC=CC=C2 |
Isomeric SMILES | CC1=NC(=CC=C1)C#CC2=CC=CC=C2 |
PubChem CID | 3025961 |
Molecular Weight | 193.24 |
PubChem CID | 3025961 |
---|---|
Wikipedia | 2-Methyl-6-(phenylethynyl)pyridine |
ChEMBL Ligand | CHEMBL66654 |
BindingDB Ligand | 50084137 |
CAS Registry No. | 96206-92-7 |
GPCRdb Ligand | MPEP |
PubChem SID | 488194193 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
L2115266 | Certificate of Analysis | Sep 19, 2023 | M127959 |
L2115279 | Certificate of Analysis | Sep 19, 2023 | M127959 |
E1716013 | Certificate of Analysis | Dec 09, 2022 | M127959 |
E2310564 | Certificate of Analysis | Dec 01, 2022 | M127959 |
E2310565 | Certificate of Analysis | Dec 01, 2022 | M127959 |
E2310566 | Certificate of Analysis | Dec 01, 2022 | M127959 |
E2310569 | Certificate of Analysis | Dec 01, 2022 | M127959 |
E2310570 | Certificate of Analysis | Dec 01, 2022 | M127959 |
E2310571 | Certificate of Analysis | Dec 01, 2022 | M127959 |
E2310572 | Certificate of Analysis | Dec 01, 2022 | M127959 |
E2310575 | Certificate of Analysis | Dec 01, 2022 | M127959 |
Solubility | DMSO 39 mg/mL Water <1 mg/mL Ethanol 39 mg/mL |
---|---|
Sensitivity | Air sensitive;Heat sensitive |
Melt Point(°C) | 47 °C |
1. Dickinson BA et al.. (2009) A novel mechanism of hippocampal LTD involving muscarinic receptor-triggered interactions between AMPARs, GRIP and liprin-alpha.. Mol Brain, 2 (18). [PMID:19534762] |
2. Gómez-Gonzalo M et al.. (2010) An excitatory loop with astrocytes contributes to drive neurons to seizure threshold.. PLoS Biol, 8 (4): (e1000352). [PMID:20405049] |
3. Min R & Nevian T. (2012) Astrocyte signaling controls spike timing-dependent depression at neocortical synapses.. Nat Neurosci, 15 (5): (746-53). [PMID:22446881] |
4. Younts TJ et al.. (2013) CA1 pyramidal cell theta-burst firing triggers endocannabinoid-mediated long-term depression at both somatic and dendritic inhibitory synapses.. J Neurosci, 33 (34): (13743-57). [PMID:23966696] |
5. Droste D et al.. (2017) Ca2+-permeable AMPA receptors in mouse olfactory bulb astrocytes.. Sci Rep, 7 (44817). [PMID:28322255] |
6. Ran I et al.. (2012) CREB-dependent transcriptional control and quantal changes in persistent long-term potentiation in hippocampal interneurons.. J Neurosci, 32 (18): (6335-50). [PMID:22553039] |
7. Shin JH et al.. (2009) Depolarization-induced slow current in cerebellar Purkinje cells does not require metabotropic glutamate receptor 1.. Neuroscience, 162 (3): (688-93). [PMID:19409231] |
8. Yang Y & Xu-Friedman MA. (2015) Different pools of glutamate receptors mediate sensitivity to ambient glutamate in the cochlear nucleus.. J Neurophysiol, 113 (10): (3634-45). [PMID:25855696] |
9. Bragina L et al.. (2015) Differential expression of metabotropic glutamate and GABA receptors at neocortical glutamatergic and GABAergic axon terminals.. Front Cell Neurosci, 9 (345). [PMID:26388733] |
10. Nasrallah C et al.. (2018) Direct coupling of detergent purified human mGlu5 receptor to the heterotrimeric G proteins Gq and Gs.. Sci Rep, 8 (4407). [PMID:29535347] |
11. Krishnan B et al.. (2011) Dopamine-induced plasticity, phospholipase D (PLD) activity and cocaine-cue behavior depend on PLD-linked metabotropic glutamate receptors in amygdala.. PLoS One, 6 (9): (e25639). [PMID:21980514] |
12. Chiu CQ et al.. (2010) Dopaminergic modulation of endocannabinoid-mediated plasticity at GABAergic synapses in the prefrontal cortex.. J Neurosci, 30 (21): (7236-48). [PMID:20505090] |
13. Andlauer TF et al.. (2014) Drep-2 is a novel synaptic protein important for learning and memory.. Elife, 3 [PMID:25392983] |
14. Ster J et al.. (2011) Enhancement of CA3 hippocampal network activity by activation of group II metabotropic glutamate receptors.. Proc Natl Acad Sci U S A, 108 (24): (9993-7). [PMID:21628565] |
15. Li Y et al.. (2012) Epileptic stimulus increases Homer 1a expression to modulate endocannabinoid signaling in cultured hippocampal neurons.. Neuropharmacology, 63 (6): (1140-9). [PMID:22814532] |
16. Li Y et al.. (2013) Epileptiform stimulus increases Homer 1a expression to modulate synapse number and activity in hippocampal cultures.. J Neurophysiol, 109 (6): (1494-504). [PMID:23274309] |
17. Chanda S & Xu-Friedman MA. (2011) Excitatory modulation in the cochlear nucleus through group I metabotropic glutamate receptor activation.. J Neurosci, 31 (20): (7450-5). [PMID:21593328] |
18. Špirková A et al.. (2022) Glutamate can act as a signaling molecule in mouse preimplantation embryos†.. Biol Reprod, 107 (4): (916-927). [PMID:35746896] |
19. Li DP & Pan HL. (2010) Increased group I metabotropic glutamate receptor activity in paraventricular nucleus supports elevated sympathetic vasomotor tone in hypertension.. Am J Physiol Regul Integr Comp Physiol, 299 (2): (R552-61). [PMID:20519363] |
20. Colavita M et al.. (2016) Layer-specific potentiation of network GABAergic inhibition in the CA1 area of the hippocampus.. Sci Rep, 6 (28454). [PMID:27345695] |
21. Liu MG et al.. (2013) Long-term potentiation of synaptic transmission in the adult mouse insular cortex: multielectrode array recordings.. J Neurophysiol, 110 (2): (505-21). [PMID:23636718] |
22. Mares P et al.. (2010) Metabotropic glutamate receptors as a target for anticonvulsant and anxiolytic action in immature rats.. Epilepsia, 51 Suppl 3 (24-6). [PMID:20618395] |
23. Jo J et al.. (2010) Muscarinic receptors induce LTD of NMDAR EPSCs via a mechanism involving hippocalcin, AP2 and PSD-95.. Nat Neurosci, 13 (10): (1216-24). [PMID:20852624] |
24. Ledonne A et al.. (2014) Neuregulin 1 signalling modulates mGluR1 function in mesencephalic dopaminergic neurons.. Mol Psychiatry, [PMID:25266126] |
25. Molina-Obando S et al.. (2019) ON selectivity in the Drosophila visual system is a multisynaptic process involving both glutamatergic and GABAergic inhibition.. Elife, 8 [PMID:31535971] |
26. Ran I et al.. (2009) Persistent transcription- and translation-dependent long-term potentiation induced by mGluR1 in hippocampal interneurons.. J Neurosci, 29 (17): (5605-15). [PMID:19403827] |
27. Habbas S et al.. (2011) Purinergic signaling in the cerebellum: Bergmann glial cells express functional ionotropic P2X7 receptors.. Glia, 59 (12): (1800-12). [PMID:21830236] |
28. Li JQ et al.. (2010) Regulation of increased glutamatergic input to spinal dorsal horn neurons by mGluR5 in diabetic neuropathic pain.. J Neurochem, 112 (162-72). [PMID:19840219] |
29. Latif-Hernandez A et al.. (2016) Separate Ionotropic and Metabotropic Glutamate Receptor Functions in Depotentiation vs. LTP: A Distinct Role for Group1 mGluR Subtypes and NMDARs.. Front Cell Neurosci, 10 (252). [PMID:27872582] |
30. Qi Y et al.. (2012) Switching off LTP: mGlu and NMDA Receptor-Dependent Novelty Exploration-Induced Depotentiation in the Rat Hippocampus.. Cereb Cortex, [PMID:22490551] |
31. Brown JT et al.. (2011) Synaptic activation of mGluR1 generates persistent depression of a fast after-depolarizing potential in CA3 pyramidal neurons.. Eur J Neurosci, 33 (5): (879-89). [PMID:21269340] |