JNJ 16259685

Name: JNJ 16259685
Brand: Tocris Bioscience
SKU: 2333

Tocris Bioscience, part of Bio-Techne | Catalog # 2333

Citations (95)

COA / SDS

Highly potent, mGlu1-selective non-competitive antagonist

Key Product Details

Description:	Highly potent, mGlu₁-selective non-competitive antagonist
Chemical Name:	(3,4-Dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-(cis-4-methoxycyclohexyl)-methanone
Purity:	≥98% (HPLC)
Molecular Weight:	325.41

View Full Technical Details for JNJ 16259685

Technical Data
Citations

Biological Activity for JNJ 16259685

JNJ 16259685 is a sub-nanomolar potent, non-competitive mGlu₁ antagonist (K_i = 0.34 nM). Inhibits glutamate-induced Ca²⁺ response at the human mGlu₁ receptor with an IC₅₀ value of 0.55 nM. Selective over mGlu₅ (> 400-fold) and displays no activity at mGlu₂, mGlu₃, mGlu₄, mGlu₆, AMPA or NMDA receptors (IC₅₀ > 10 μM). Centrally active following systemic administration.

Compound Libraries for JNJ 16259685

JNJ 16259685 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for JNJ 16259685

M. Wt	325.41
Formula	C₂₀H₂₃NO₃
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	409345-29-5
PubChem ID	11313361
InChi Key	QOTAQTRFJWLFCR-UHFFFAOYSA-N
Smiles	O=[C@@]([C@@H]4CC[C@H](OC)CC4)C(C=C3)=CC1=C3N=C(OCCC2)C2=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 JNJ 16259685

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	ethanol	32.54	100
	DMSO	8.14	25

Preparing Stock Solutions for JNJ 16259685

The following data is based on the product molecular weight 325.41.

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	3.07 mL	15.37 mL	30.73 mL
5 mM	0.61 mL	3.07 mL	6.15 mL
10 mM	0.31 mL	1.54 mL	3.07 mL
50 mM	0.06 mL	0.31 mL	0.61 mL

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References for JNJ 16259685

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

Xie Effects of mGluR1 antagonism in the dorsal hippocampus on drug context-induced reinstatement of cocaine-seeking behavior in rats. Psychopharmacology (Berl). 2010 PMID: 19847405
Mabire Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists. J.Med.Chem. 2005 PMID: 15771457
Steckler Metabotropic glutamate receptor 1 blockade impairs acquisition and retention in a spatial water maze task. Behav.Brain Res. 2005 PMID: 16043241
Lavreysen JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist. Neuropharmacology 2004 PMID: 15555631