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Description: mGlu5 antagonist; also positive allosteric modulator at mGlu4 receptors
Chemical Name: 2-Methyl-6-(2-phenylethenyl)pyridine
Biological Activity
A highly selective non-competitive antagonist for the metabotropic glutamate mGlu5 receptor subtype; displays an IC50 value of 0.3 μM at hmGlu5, compared with > 100 μM at hmGlu1b, hmGlu2, hmGlu6, hmGlu7 and hmGlu8. Centrally active upon systemic administration in vivo. Positive allosteric modulator at mGlu4 receptors.
Technical Data
| M. Wt | 195.26 |
| Formula | C14H13N |
| Storage | Desiccate at +4°C |
| CAS Number | 6266-99-5 |
| PubChem ID | 4713 |
| InChI Key | QFWCYNPOPKQOKV-UHFFFAOYSA-N |
| Smiles | CC1=NC(\C=C\C2=CC=CC=C2)=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 195.26. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 5.12 mL | 25.61 mL | 51.21 mL |
| 5 mM | 1.02 mL | 5.12 mL | 10.24 mL |
| 10 mM | 0.51 mL | 2.56 mL | 5.12 mL |
| 50 mM | 0.1 mL | 0.51 mL | 1.02 mL |
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References
References are publications that support the biological activity of the product.
Chapman et al (2000) Anticonvulsant activity of two metabotropic glutamate group I antagonists selective for the mGlu5 receptor: 2-methyl-6-(phenylethynyl)-pyridine (MPEP), and (E)-6-methyl-2-styryl-pyridine (SIB 1893). Neuropharmacology 39 1567 PMID: 10854901
Mathiesen et al (2003) Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP. Br.J.Pharmacol. 138 1026 PMID: 12684257
Varney et al (1999) SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5. J.Pharmacol.Exp.Ther. 290 170 PMID: 10381773
If you know of a relevant reference for SIB 1893, please let us know.
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Keywords: SIB 1893, SIB 1893 supplier, Positive, allosteric, modulators, mGlu4, mGluR4, mGlu5, mGluR5, antagonist, positive, Group, III, Receptors, Glutamate, Metabotropic, I, SIB1893, PAM, (Metabotropic), 1214, Tocris Bioscience
2 Citations for SIB 1893
Citations are publications that use Tocris products. Selected citations for SIB 1893 include:
Mathiesen et al (2003) Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP. Br J Pharmacol 138 1026 PMID: 12684257
Edri et al (2015) Analysing human neural stem cell ontogeny by consecutive isolation of Notch active neural progenitors. Nat Commun 6 6500 PMID: 25799239
Do you know of a great paper that uses SIB 1893 from Tocris? Please let us know.
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