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Submit ReviewLSN 2463359
Description: Potent and selective positive allosteric modulator of mGlu5 receptors
Chemical Name: N-(1-Methylethyl)-5-[2-(4-pyridinyl)ethynyl]-2-pyridinecarboxamide
Purity: ≥99% (HPLC)
Biological Activity for LSN 2463359
LSN 2463359 is a potent and selective positive allosteric modulator at the mGlu5 receptor (EC50 = 24 nM). Has no activity at mGlu1-4, mGlu8 and GABAB receptors. Reverses methylazoxymethanol acetate (MAM)-induced deficits in reversal learning memory and normalizes SDZ 220-581 and RO 63-1908-induced alterations in instrumental responses in rat models. Promotes wakefulness in vivo. Brain penetrant and orally active.
Technical Data for LSN 2463359
| M. Wt | 265.31 |
| Formula | C16H15N3O |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1401031-52-4 |
| PubChem ID | 72551298 |
| InChI Key | STAFRSGTRKNXHF-UHFFFAOYSA-N |
| Smiles | O=C(NC(C)C)C(C=C2)=NC=C2C#CC1=CC=NC=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 for LSN 2463359
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 26.53 | 100 | |
| ethanol | 5.31 | 20 |
Preparing Stock Solutions for LSN 2463359
The following data is based on the product molecular weight 265.31. 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 | 3.77 mL | 18.85 mL | 37.69 mL |
| 5 mM | 0.75 mL | 3.77 mL | 7.54 mL |
| 10 mM | 0.38 mL | 1.88 mL | 3.77 mL |
| 50 mM | 0.08 mL | 0.38 mL | 0.75 mL |
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Product Datasheets for LSN 2463359
References for LSN 2463359
References are publications that support the biological activity of the product.
Gastambide et al (2012) Selective remediation of reversal learning deficits in the neurodevelopmental MAM model of schizophrenia by a novel mGlu5 positive allosteric modulator. Neuropsychopharmacology 37 1057 PMID: 22129780
Gilmour et al (2013) In vitro characterisation of the novel positive allosteric modulators of the mGlu5 receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat. Neuropharmacology 64 224 PMID: 22884720
Gastambide et al (2013) The mGlu5 positive allosteric modulator LSN2463359 differentially modulates motor, instrumental and cognitive effects of NMDA receptor antagonists in the rat. Neuropharmacology 64 240 PMID: 22884612
If you know of a relevant reference for LSN 2463359, please let us know.
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Keywords: LSN 2463359, LSN 2463359 supplier, LSN2463359, potent, selective, positive, allosteric, modulator, PAM, MGLU5, brain, penetrant, orally, active, schizophrenia, Glutamate, (Metabotropic), Group, I, Receptors, 5275, Tocris Bioscience
Citations for LSN 2463359
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Metabotropic Glutamate Receptors Scientific Review
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