Home Tools

JNJ16259685

Catalog No. T5512 CAS 409345-29-5

Synonyms: .TN.T 16259685

JNJ16259685 (TN.T 16259685) is a selective mGluR1 antagonist, and inhibits the synaptic activation of mGluR1 in a concentration-dependent manner with IC50 of 19 nM.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

JNJ16259685, CAS 409345-29-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 41.00
2 mg	In stock	$ 59.00
5 mg	In stock	$ 92.00
10 mg	In stock	$ 143.00
25 mg	In stock	$ 308.00
50 mg	In stock	$ 472.00
100 mg	In stock	$ 689.00
1 mL * 10 mM (in DMSO)	In stock	$ 102.00

Bulk Inquiry

Select Batch

Purity: 99.39%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	JNJ16259685 (TN.T 16259685) is a selective mGluR1 antagonist, and inhibits the synaptic activation of mGluR1 in a concentration-dependent manner with IC50 of 19 nM.
Targets&IC50	mGluR1:19 nM
In vitro	JNJ16259685 non-competitively inhibited glutamate-induced Ca2+ mobilization with IC50 values of 3.24+/-1.00 and 1.21+/-0.53 nM, respectively, while showing a much lower potency at the rat and human mGlu5a receptor.?JNJ16259685 inhibited [3H]1-(3,4-dihydro-2H-pyrano[2,3-b]quinolin-7-yl)-2-phenyl-1-ethanone ([3H]R214127) binding to membranes prepared from cells expressing rat mGlu1a receptors with a Ki of 0.34+/-0.20 nM.?JNJ16259685 showed no agonist, antagonist or positive allosteric activity toward rat mGlu2, -3, -4 or -6 receptors at concentrations up to 10 microM and did not bind to AMPA or NMDA receptors, or to a battery of other neurotransmitter receptors, ion channels and transporters.?In primary cerebellar cultures, JNJ16259685 inhibited glutamate-mediated inositol phosphate production with an IC50 of 1.73+/-0.40 nM.?Subcutaneously administered JNJ16259685 exhibited high potencies in occupying central mGlu1 receptors in the rat cerebellum and thalamus ( ED50=0.040 and 0.014 mg/kg, respectively)[3].
In vivo	JNJ16259685, a selective mGluR1 antagonist (negative allosteric modulator), was tested in assays of motor skill, and motor learning in rats and mice.?JNJ16259685 produced very minimal effects on locomotor activity and posture up to a dose of 30 mg/kg.?Motor skill was unaffected for well-learned tasks (up to 30 mg/kg) in rats, but impaired in mice.?Both rats and mice rats were profoundly impaired (0.3 mg/kg) in the acquisition of a novel motor skill (rotarod).?These results implicate the mGluR1 receptor in the acquisition of novel motor skills.?JNJ16259685 dramatically reduced rearing behavior, exploration of a novel environment and lever pressing for a food reward (rat: 0.3 mg/kg;?mouse: 1 mg/kg).?JNJ16259685 (30 mg/kg) had no effect on reflexive startle responses to loud auditory stimuli or foot shock in mice[1].

Synonyms	.TN.T 16259685
Molecular Weight	325.4
Formula	C20H23NO3
CAS No.	409345-29-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (307.31 mM)

References and Literature

1. Hodgson RA, et al. Characterization of the selective mGluR1 antagonist, JNJ16259685, in rodent models of movement and coordination. Pharmacol Biochem Behav. 2011 Apr;98(2):181-7. 2. Navarro JF,et al. JNJ16259685, a selective mGlu1 antagonist, suppresses isolation-induced aggression in male mice. Eur J Pharmacol. 2008 May 31;586(1-3):217-20. 3. Lavreysen H,et al. JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist. Neuropharmacology. 2004 Dec;47(7):961-72.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Neurodegenerative Disease Compound Library Neuronal Signaling Compound Library NO PAINS Compound Library Covalent Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max Neurotransmitter Receptor Compound Library Anti-Parkinson's Disease Compound Library

Related Products

Related compounds with same targets

SIB-1757 GYKI 53655 hydrochloride PHCCC L-Cysteic acid monohydrate (R)-3,4-DCPG HCl Pomaglumetad methionil hydrochloride XAP044 Basimglurant

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

JNJ16259685 409345-29-5 Neuroscience GluR .TN.T 16259685 JNJ-16259685 inhibit Inhibitor mGluR .TN.T16259685 .TN.T-16259685 JNJ 16259685 Metabotropic glutamate receptors inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.