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Home / Biochemicals / Small Molecules

NPS 2390

SKU : BHB21300248

A Potent and Selective Antagonist of mGluR1 and mGluR5 Receptors

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Mfr.No.	N-340, N-340_10 mg, N-340_25 mg, N-340_5 mg, N-340_50 mg
Description	NPS 2390 (#N-340) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C19H21N3O.
Background	NPS 2390, a quinoxaline derivative, is a synthetic, potent, selective and non-competitive antagonist of group I metabotropic glutamate receptors comprising mGluR1 and mGluR5 receptors with IC50 values of 5.2 and 8.2 nM respectively7. The compound shows very low affinity towards other mGluR receptors.Several studies suggest that NPS 2390 acts on a site that is different from the glutamate binding pocket. It is likely that the compound acts at the transmembrane segment VII region of the receptors1-3.Metabotropic glutamate receptors (mGluRs) are G protein coupled receptors (GPCR) that play an important role in synaptic plasticity and other neuro-physiological and pathological processes including a major role in central sensitization and neuropathic pain. Type 1 mGluRs are mainly found in somatodendritic domains and postsynaptically regulate neuronal excitability and synaptic transmission through several intracellular second messenger systems4,5. The mGlu1 receptors play an important role in motor learning and motor coordination whereas mGlu5 receptors contribute to induction of long-term potentiation and associative learning6.
Shipping	Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C
Concentration	10 nM - 1 uM.
Reconstitution	Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 uM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity
Cas Number	226878-01-9
Molecular Weight	307.4
Solubility	Up to 25 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Target	mGluR1, mGluR5 receptors
Source	Synthetic
Activity	NPS 2390, a quinoxaline derivative, is a potent and selective non-competitive antagonist of Group I mGluRs, acting on mGluR1 and mGluR5 with IC50 values of to 5.2 and 82 nM, respectively, while having no effect on mGluR2, mGluR8 and other targets at 30 uM1-3.
Country Of Origin	Israel/IL
UNSPSC Code	41116134
Application	FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay
Lead Time	1-2 Business Days
Notes	Bioassay Tested: Yes Chemical Name: N-(1-adamantyl)quinoxaline-2-carboxamide.

Purity	>98%
Form	Lyophilized powder.
Storage	Storage After Reconstitution: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles. Storage of solutions: -20°C.

Product Manual	SDS

Reference	Mabire, D. et al. (2005) J. Med. Chem. 48, 2134. Lavreysen, H. et al. (2003) Mol. Pharmacol. 63, 1082. Van Wagenen, B.C. et al. (2000) Abstr. Soc. Neurosci. Presentation No. 618, 3. O'Brien, J.A. et al. (2003) Mol. Pharmacol. 64, 731. Satow, A. et al. (2008) J. Pharmacol. Exp. Ther. 326, 577. Eom, H.S. et al. (2016) PLoS One 11, e0147538. Lu, Y.M. et al. (1996) J. Neurosci. 17, 5196. Mabire, D. et al. (2005) J. Med. Chem. 48, 2134. Lavreysen, H. et al. (2003) Mol. Pharmacol. 63, 1082. Van Wagenen, B.C. et al. (2000) Abstr. Soc. Neurosci. Presentation No. 618, 3.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300248-1	N-340_10 mg	10 mg	$117		Add to Cart
BHB21300248-2	N-340_25 mg	25 mg	$263		Add to Cart
BHB21300248-3	N-340_5 mg	5 mg	$85		Add to Cart
BHB21300248-4	N-340_50 mg	50 mg	$425		Add to Cart

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