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Home / Biochemicals / Small Molecules

JNJ 16259685

SKU : BHB21300184

A Potent and Selective Antagonist of mGluR1

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Mfr.No.	J-110, J-110_10 mg, J-110_25 mg, J-110_5 mg, J-110_50 mg
Description	JNJ 16259685 (#J-110) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C20H23NO3.
Background	JNJ 16259685 is a potent, specific, and non-competitive antagonist of mGluR1 displaying an IC50 of 19 nM1. The compound shows a much lower potency towards mGluR5 receptor1,2.Glutamate is the most abundant excitatory neurotransmitter in the central nervous system and it modulates activity of many types of synapses by activating in part metabotropic glutamate receptors (mGluRs). mGluRs consist of three groups: I, II, and III with a total of eight subtypes, mGluR1 to mGluR8.mGluR1 plays an important role in the central sensitization of pain and in various physiological functions including regulating ion channels, synaptic transmission, and synaptic plasticity2.
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	Soluble in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Cas Number	409345-29-5
Molecular Weight	325.41
Solubility	Soluble in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Target	mGluR1
Source	Synthetic
Activity	JNJ 16259685 is a potent and selective non-competitive antagonist of mGluR1 receptors, inhibiting human mGluR1 and mGluR5 mediated glutamate-induced Ca2+ mobilization with IC50 values of 1.21 nM and 28.3 uM, respectively, whilst having no effect on a range of other receptor subtypes at over 10 uM1.It is systemically active, occupying central mGluR1 receptors in the rat cerebellum and thalamus (ED50 = 40 and 14 ug/kg, respectively) when administered subcutaneously1. JNJ 16259685 inhibits synaptic activation of mGluR1 in Purkinje cells in cerebellar slices with IC50 of 19 nM2.
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: 3,4-dihydro-2H-pyrano(2,3-b)quinolin-7-yl-(4-methoxycyclohexyl)methanone.

Purity	>97%
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	Fukunaga, I. et al. (2007) Br. J. Pharmacol. 151, 870. Zheng, G.Z. et al. (2005) J. Med. Chem. 48, 7374. Lavreysen, H. et al. (2004) Neuropharmacology 47, 961. Fukunaga, I. et al. (2007) Br. J. Pharmacol. 151, 870.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300184-1	J-110_10 mg	10 mg	$168		Add to Cart
BHB21300184-2	J-110_25 mg	25 mg	$390		Add to Cart
BHB21300184-3	J-110_5 mg	5 mg	$117		Add to Cart
BHB21300184-4	J-110_50 mg	50 mg	$680		Add to Cart

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