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Home / Biochemicals / Small Molecules

LY456066

SKU : BHB21300210

A Potent Antagonist of mGluR1 Receptors

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Mfr.No.	L-240, L-240_10 mg, L-240_25 mg, L-240_5 mg, L-240_50 mg
Description	LY456066 (#L-240) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C19H23N3OS.
Pubchem Cid	9840951
Synonyms	Synthetic
Background	LY456066 is a selective, negative allosteric modulator of mGluR1 receptors. The compound demonstrates high potent antagonistic activities toward both rat and human mGluR1 receptor with an IC50 value of 28 nM for human mGluR1 receptors expressed in Chinese hamster ovary cells1,2. Several studies have suggested that LY456066 may bind to a site at the mGluR1 receptor that could represent a conserved negative allosteric regulatory domain3.Metabotropic glutamate receptors (mGluRs) are G-protein coupled receptors (GPCR) that play an important role in synaptic plasticity and other neurophysiological and pathological processes including a major role in central sensitization and neuropathic pain. Type 1 mGluRs are mainly found on post-synaptic neurons and are known to affect the fate of neuronal progenitor cells and neural stem cell and the formation of the hippocampus4.
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	1 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
Molecular Weight	341.47
Solubility	Up to 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Target	mGluR1
Activity	LY456066 is a potent antagonist of mGluR1 receptors. It inhibits human mGluR1 receptors expressed in CHO cells with an IC50 of 28 nM1.
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: 2-((4-(2,3-dihydro-1H-inden-2-ylamino)-5,6,7,8-tetrahydroquinazolin-2-yl)sulfanyl)ethanol.

Purity	>99%
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	Fukuda. J. et al. (2009) Neuropharmacology 57, 438. Suzuki, G. et al. (2007) J. Pharmacol. Exp. Ther. 321, 1144. Tsui, H.T. et al. (2002) Soc. Neurosci. Meet. Abstract No. 247.3. Eom, H.S. et al. (2016) PLoS One 11, e0147538. Fukuda, J. et al. (2009) Neuropharmacology 57, 438.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300210-1	L-240_10 mg	10 mg	$235		Add to Cart
BHB21300210-2	L-240_25 mg	25 mg	$468		Add to Cart
BHB21300210-3	L-240_5 mg	5 mg	$168		Add to Cart
BHB21300210-4	L-240_50 mg	50 mg	$843		Add to Cart

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