LSN 2463359

Name: LSN 2463359
Brand: Tocris Bioscience
SKU: 5275

Tocris Bioscience, part of Bio-Techne | Catalog # 5275

COA / SDS

Potent and selective positive allosteric modulator of mGlu5 receptors

Key Product Details

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)
Molecular Weight:	265.31

View Full Technical Details for LSN 2463359

Technical Data
Citations

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 mGlu_1-4, mGlu₈ and GABA_B 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 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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References for LSN 2463359

References are publications that support the biological activity of the product.

Gilmour 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 2013 PMID: 22884720
Gastambide The mGlu₅ positive allosteric modulator LSN2463359 differentially modulates motor, instrumental and cognitive effects of NMDA receptor antagonists in the rat. Neuropharmacology 2013 PMID: 22884612
Gastambide Selective remediation of reversal learning deficits in the neurodevelopmental MAM model of schizophrenia by a novel mGlu5 positive allosteric modulator. Neuropsychopharmacology 2012 PMID: 22129780