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MFZ 10-7

Negative allosteric modulator at mGlu5 CAS# 1224431-15-5

MFZ 10-7

Catalog No. BCC6180----Order now to get a substantial discount!

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MFZ 10-7: 5mg $104 In Stock
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Chemical structure

MFZ 10-7

3D structure

Chemical Properties of MFZ 10-7

Cas No. 1224431-15-5 SDF Download SDF
PubChem ID 90488944 Appearance Powder
Formula C15H10ClFN2 M.Wt 272.7
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO and to 100 mM in ethanol
Chemical Name 3-fluoro-5-[2-(6-methylpyridin-2-yl)ethynyl]benzonitrile;hydrochloride
SMILES CC1=CC=CC(=N1)C#CC2=CC(=CC(=C2)F)C#N.Cl
Standard InChIKey WRHOKQFFLQKKNL-UHFFFAOYSA-N
Standard InChI InChI=1S/C15H9FN2.ClH/c1-11-3-2-4-15(18-11)6-5-12-7-13(10-17)9-14(16)8-12;/h2-4,7-9H,1H3;1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of MFZ 10-7

DescriptionHigh affinity negative allosteric modulator at the mGlu5 receptor (Ki = 0.67 nM). Potently inhibits mGlu5 glutamate-mediated calcium mobilization (IC50 = 1.22 nM). Inhibits cocaine-taking and cocaine-seeking behavior in rats.

MFZ 10-7 Dilution Calculator

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MFZ 10-7 Molarity Calculator

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Preparing Stock Solutions of MFZ 10-7

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.667 mL 18.3352 mL 36.6703 mL 73.3407 mL 91.6758 mL
5 mM 0.7334 mL 3.667 mL 7.3341 mL 14.6681 mL 18.3352 mL
10 mM 0.3667 mL 1.8335 mL 3.667 mL 7.3341 mL 9.1676 mL
50 mM 0.0733 mL 0.3667 mL 0.7334 mL 1.4668 mL 1.8335 mL
100 mM 0.0367 mL 0.1834 mL 0.3667 mL 0.7334 mL 0.9168 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on MFZ 10-7

A novel mGluR5 antagonist, MFZ 10-7, inhibits cocaine-taking and cocaine-seeking behavior in rats.[Pubmed:24001208]

Addict Biol. 2014 Mar;19(2):195-209.

Pre-clinical studies suggest that negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 5 (mGluR5), including 2-methyl-6-(phenylethynyl)pyridine (MPEP), 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) and fenobam are highly effective in attenuating drug-taking and drug-seeking behaviors. However, both MPEP and MTEP have no translational potential for use in humans because of their off-target effects and short half-lives. Here, we report that 3-fluoro-5-[(6-methylpyridin-2-yl)ethynyl]benzonitrile (MFZ 10-7), a novel mGluR5 NAM, is more potent and selective than MPEP, MTEP and fenobam in both in vitro binding and functional assays. Similar to MTEP, intraperitoneal administration of MFZ 10-7 inhibited intravenous cocaine self-administration, cocaine-induced reinstatement of drug-seeking behavior and cocaine-associated cue-induced cocaine-seeking behavior in rats. Although MFZ 10-7 and MTEP lowered the rate of oral sucrose self-administration, they did not alter total sucrose intake. Further, MFZ 10-7 appeared to be more potent than MTEP in inducing downward shifts in the cocaine dose-response curve, but less effective than MTEP in attenuating sucrose-induced reinstatement of sucrose-seeking behavior. MFZ 10-7 and MTEP had no effect on basal locomotor behavior. These findings not only provide additional evidence supporting an important role for mGluR5 in cocaine reward and addiction, but also introduce a new tool for both in vitro and in vivo investigations with which to further characterize this role.

Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation.[Pubmed:22924094]

ACS Med Chem Lett. 2012 Jul 12;3(7):544-549.

Negative allosteric modulators (NAMs) of metabotropic glutamate receptor subtype 5 (mGluR5) have shown promising results in preclinical models for anxiety and drug abuse. Here we describe a series of aryl-substituted alkynyl analogues of the prototypic mGluR5 NAM 2-methyl-6-(phenylethynyl)pyridine (MPEP, 1). Displacement of [(3)H]1 binding in rat brain membranes showed that several of these novel compounds displayed high affinity binding (K(i) < 10 nM) for mGluR5, with up to a 24-fold increase in affinity over 1. Replacements of the 2-position Me on the pyridyl ring of 1 along with various 3'-CN, 5'-substitutions were generally well tolerated. All of the active analogues in this series had cLogP values in the 2-5 range and displayed inverse agonist characteristics in an ELISA-based assay of G(q)alpha-mediated IP3 production. Compounds 7i and 7j produced in vivo effects in mouse models of anxiety-like behaviors more potently than 1 or 3-((2-methyl-1,3-thiazol-4-yl)ethynyl)pyridine (MTEP, 2), supporting their utility as in vivo tools.

Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series.[Pubmed:21546249]

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3243-7.

We report the synthesis of four series of 3,5-disubstituted-phenyl ligands targeting the metabotropic glutamate receptor subtype 5: (2-methylthiazol-4-yl)ethynyl (1a-j,), (6-methylpyridin-2-yl)ethynyl (2a-j), (5-methylpyridin-2-yl)ethynyl (3a-j,), and (pyridin-2-yl)ethynyl (4a-j,). The compounds were evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro assay. All compounds were found to be full antagonists and exhibited low nanomolar to subnanomolar activity.

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