ADX 10059 hydrochlorideNegative allosteric modulator at mGlu5 CAS# 757949-98-7 |
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| Cas No. | 757949-98-7 | SDF | Download SDF |
| PubChem ID | 18454771 | Appearance | Powder |
| Formula | C15H14ClFN2 | M.Wt | 276.74 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 25 mM in water and to 100 mM in DMSO | ||
| Chemical Name | 2-[2-(3-fluorophenyl)ethynyl]-4,6-dimethylpyridin-3-amine;hydrochloride | ||
| SMILES | CC1=CC(=NC(=C1N)C#CC2=CC(=CC=C2)F)C.Cl | ||
| Standard InChIKey | BDXXMGYKLQZXOU-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C15H13FN2.ClH/c1-10-8-11(2)18-14(15(10)17)7-6-12-4-3-5-13(16)9-12;/h3-5,8-9H,17H2,1-2H3;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. |
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| 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. |
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| 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. | ||
| Description | Reported to be a negative allosteric modulator at the mGlu5 receptor. Analog of MPEP. |
ADX 10059 hydrochloride Dilution Calculator
ADX 10059 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.6135 mL | 18.0675 mL | 36.135 mL | 72.27 mL | 90.3375 mL |
| 5 mM | 0.7227 mL | 3.6135 mL | 7.227 mL | 14.454 mL | 18.0675 mL |
| 10 mM | 0.3614 mL | 1.8068 mL | 3.6135 mL | 7.227 mL | 9.0338 mL |
| 50 mM | 0.0723 mL | 0.3614 mL | 0.7227 mL | 1.4454 mL | 1.8068 mL |
| 100 mM | 0.0361 mL | 0.1807 mL | 0.3614 mL | 0.7227 mL | 0.9034 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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6-Aryl-3-pyrrolidinylpyridines as mGlu5 receptor negative allosteric modulators.[Pubmed:21757343]
Bioorg Med Chem Lett. 2011 Aug 15;21(16):4891-9.
A series of 6-aryl-3-pyrrolidinylpyridine analogs was explored as structurally novel negative allosteric modulators of the mGlu5 receptor lacking an alkyne or oxadiazole moiety. Compounds in this series were characterized by tractable SAR, good in vitro potencies and brain penetration in rodents.
Glutamatergic fine tuning with ADX-10059: a novel therapeutic approach for migraine?[Pubmed:20218930]
Expert Opin Investig Drugs. 2010 Apr;19(4):555-61.
IMPORTANCE OF THE FIELD: Migraine is an episodic, substantially inherited brain disorder affecting 15% of adults in Western Europe and North America, and is one of the commonest reasons for patients to see their physicians. While the World Health Organization considers that severe migraine can be as disabling as quadriplegia, unfortunately the condition remains undertreated. Until the 1990s, specific migraine therapies were limited to ergot derivatives. AREAS COVERED IN THIS REVIEW: The triptans, serotonin 5-HT(1B/1D) receptor agonists, revolutionized the acute management of migraine patients. However, although the triptans are generally effective and safe, not all patients can take them and many do not respond especially to oral therapies. Recently, progress has been made on the therapeutic front, particularly with new acute treatments. This review will focus on the therapeutic potential of ADX10059, a metabotropic glutamate receptor 5, negative allosteric modulator (mGluR5 NAM), in migraine. Data from a proof-of-concept study in episodic migraineurs demonstrated a significant improvement following acute treatment. A large European multicenter, randomized, double-blind, placebo-controlled, parallel-group, dose-ranging study is currently investigating the efficacy, safety and tolerability of the compound for migraine prevention. WHAT THE READER WILL GAIN: The reader will have the basic principles of migraine management and the potential for glutamate-targeted approaches. TAKE HOME MESSAGE: Targeting glutamatergic transmission in migraine may provide a novel preventive therapy that is effective and well-tolerated.
A proof-of-concept study evaluating the effect of ADX10059, a metabotropic glutamate receptor-5 negative allosteric modulator, on acid exposure and symptoms in gastro-oesophageal reflux disease.[Pubmed:19460767]
Gut. 2009 Sep;58(9):1192-9.
BACKGROUND: In preclinical models, antagonism of metabotropic glutamate receptor 5 (mGluR5) reduces transient lower oesophageal sphincter relaxations (TLOSRs) and increases LOS pressure. This study evaluated the effect of ADX10059, a potent, selective, negative allosteric modulator of mGluR5, on oesophageal pH-metry and clinical symptoms in GORD. METHODS: Two groups of patients with GORD (n = 12 per group) underwent 24-h oesophageal pH-metry on two sequential treatment days. The patients received oral placebo three times daily (tds) 30 min before a high-fat meal on Day 1 and oral ADX10059 50 mg (Group 1) or 250 mg (Group 2) tds 30 min before a high-fat meal on Day 2. The primary variable was acid exposure (%time pH<4). Secondary variables included number and duration of reflux episodes, number and duration of symptomatic episodes and symptoms recorded in diaries. Comparisons were made for Day 2 (active) versus Day 1 (placebo) treatment and for Group 1 versus Group 2. RESULTS: ADX10059 250 mg tds significantly decreased the percentage of time with pH<4 from 7.2% to 3.6% (p = 0.01). ADX10059 250 mg tds reduced pH-metry-measured oesophageal acid exposure, throughout the 24 h period, nocturnally and postprandially, and significantly reduced the number and duration of symptomatic reflux episodes (p = 0.03). ADX10059 50 mg tds was not significantly superior to placebo. ADX10059 was generally well tolerated. CONCLUSION: The mGluR5 negative allosteric modulator ADX10059 reduced acid reflux which was associated with improvement in clinical symptoms in patients with GORD. ADX10059 appears to have a potential role in the clinical management of GORD.
