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Tocris/LSN 2463359/5275/10/10 mg

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货号: 5275/10

品牌: Tocris

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Description: Potent and selective positive allosteric modulator at mGlu₅

Chemical Name: N-(1-Methylethyl)-5-[2-(4-pyridinyl)ethynyl]-2-pyridinecarboxamide

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

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.

Compound Libraries

LSN 2463359 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	26.53	100
	ethanol	5.31	20

Preparing Stock Solutions

The following data is based on the product molecular weight 265.31. 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	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

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

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

Keywords: LSN 2463359, supplier, LSN2463359, potent, selective, positive, allosteric, modulator, PAM, MGLU5, brain, penetrant, orally, active, schizophrenia, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience

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