SIB 1893
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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 100 mM in DMSO |
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 solvent 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 products' biological activity.
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: Positive allosteric modulators mGlu4 mGluR4 mGlu5 mGluR5 antagonist positive Group III Receptors Glutamate Metabotropic I SIB1893 Glutamate (Metabotropic) Group I Receptors
2 Citations for SIB 1893
Citations are publications that use Tocris products. Selected citations for SIB 1893 include:
Edri et al (2015) Analysing human neural stem cell ontogeny by consecutive isolation of Notch active neural progenitors. Nat Commun 6 6500 PMID: 25799239
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
Do you know of a great paper that uses SIB 1893 from Tocris? If so please let us know.
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