VU 0361737MGlu4 receptor allosteric modulator CAS# 1161205-04-4 |
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Quality Control & MSDS
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| Cas No. | 1161205-04-4 | SDF | Download SDF |
| PubChem ID | 44191096 | Appearance | Powder |
| Formula | C13H11ClN2O2 | M.Wt | 262.69 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | ML-128 | ||
| Solubility | DMSO : ≥ 43 mg/mL (163.69 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | N-(4-chloro-3-methoxyphenyl)pyridine-2-carboxamide | ||
| SMILES | COC1=C(C=CC(=C1)NC(=O)C2=CC=CC=N2)Cl | ||
| Standard InChIKey | ARYUXFNGXHNNDM-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C13H11ClN2O2/c1-18-12-8-9(5-6-10(12)14)16-13(17)11-4-2-3-7-15-11/h2-8H,1H3,(H,16,17) | ||
| 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 | Selective positive allosteric modulator at mGlu4 receptors (EC50 values are 240 and 110 nM at human and rat receptors respectively). Inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. Brain penetrant. |
VU 0361737 Dilution Calculator
VU 0361737 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.8068 mL | 19.0338 mL | 38.0677 mL | 76.1354 mL | 95.1692 mL |
| 5 mM | 0.7614 mL | 3.8068 mL | 7.6135 mL | 15.2271 mL | 19.0338 mL |
| 10 mM | 0.3807 mL | 1.9034 mL | 3.8068 mL | 7.6135 mL | 9.5169 mL |
| 50 mM | 0.0761 mL | 0.3807 mL | 0.7614 mL | 1.5227 mL | 1.9034 mL |
| 100 mM | 0.0381 mL | 0.1903 mL | 0.3807 mL | 0.7614 mL | 0.9517 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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VU0361737 is a selective, positive allosteric modulator and brain-permeable for mGLuR4 (mGlu4 receptor), (EC₅₀ = 240 and 110 nM for human and rat receptors respectively), >50 fold selectivity over other mGluR subtypes. Inactive at mGluR-1, mGluR-2, mGluR-3, mGluR-6 and mGluR-7 receptors and showed weak activity at mGluR-5 and mGluR-8 receptors. [1]
The mGluR (metabotropic glutamate receptor) is a group of G-protein coupled receptors and is active through an indirect metabotropic process. mGLuR4 are invoinved in Parkinson as it decrease GABAerigic transmission at inhibitory striato-pallidal synapse with the basal ganglia.[1][2]
Following the administration of VU0361737 into rat intraperitoneally (10mg/kg), the amount of compound present in brain and plasma was determined at 0.5, 1 and 8 hours. It showed a short half-life (T1/2 20 minutes) and a pronounced brain exposure (brain: plasma ratio = 4.1) [1]
References:
[1] Engers DW, Niswender CM, Weaver CD, Jadhav S, Menon UN, Zamorano R, Conn PJ, Lindsley CW, Hopkins CR. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). J Med Chem. 2009 Jul 23;52(14):4115-8.
[2] Engers DW, Field JR, Le U, Zhou Y, Bolinger JD, Zamorano R, Blobaum AL, Jones CK, Jadhav S, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats. J Med Chem. 2011 Feb 24;54(4):1106-10.
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Ned Tijdschr Geneeskd. 2017;161:D861.
On 8 September 2015, flooding of the lower floors of the VU University Medical Center in Amsterdam caused serious damage to many vital technical services, such as water and power supplies. The decision was made to completely evacuate the university hospital. This paper describes the chronology and events of that day and shares a number of important lessons that were learned, in order to help readers to optimise crisis organisation in their own institutions. A serious situation or disaster can never be standardised in protocols or manuals; flexibility, improvisation and confidence in one another's expertise and commitment are therefore essential.
Why is it (also) so difficult to legislate gambling in Spain? 'Deja vu' of what occurred with alcohol.[Pubmed:27749963]
Adicciones. 2016 Oct 6;28(4):189-193.
Editorial of vol 28-4.
Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats.[Pubmed:21247167]
J Med Chem. 2011 Feb 24;54(4):1106-10.
Herein we report the discovery, synthesis, and evaluation of a series of N-(4-acetamido)-phenylpicolinamides as positive allosteric modulators of mGlu(4). Compounds from the series show submicromolar potency at both human and rat mGlu(4). In addition, pharmacokinetic studies utilizing subcutaneous dosing demonstrated good brain exposure in rats.
Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs).[Pubmed:19469556]
J Med Chem. 2009 Jul 23;52(14):4115-8.
We report the synthesis and evaluation of a series of heterobiaryl amides as positive allosteric modulators of mGluR4. Compounds 9b and 9c showed submicromolar potency at both human and rat mGluR4. In addition, both 9b and 9c were shown to be centrally penetrant in rats using nontoxic vehicles, a major advance for the mGluR4 field.
