VU 0364439Positive allosteric mGluR-4 modulator CAS# 1246086-78-1 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1246086-78-1 | SDF | Download SDF |
| PubChem ID | 46934289 | Appearance | Powder |
| Formula | C18H13Cl2N3O3S | M.Wt | 422.29 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 50 mg/mL (118.40 mM; Need ultrasonic) | ||
| Chemical Name | N-[3-chloro-4-[(2-chlorophenyl)sulfamoyl]phenyl]pyridine-2-carboxamide | ||
| SMILES | C1=CC=C(C(=C1)NS(=O)(=O)C2=C(C=C(C=C2)NC(=O)C3=CC=CC=N3)Cl)Cl | ||
| Standard InChIKey | IXHCGJXBIHHIEF-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C18H13Cl2N3O3S/c19-13-5-1-2-6-15(13)23-27(25,26)17-9-8-12(11-14(17)20)22-18(24)16-7-3-4-10-21-16/h1-11,23H,(H,22,24) | ||
| 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 | Positive allosteric modulator (PAM) of mGlu4 receptors (EC50 = 19.8 nM in vitro for human mGlu4). |
VU 0364439 Dilution Calculator
VU 0364439 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.368 mL | 11.8402 mL | 23.6804 mL | 47.3608 mL | 59.201 mL |
| 5 mM | 0.4736 mL | 2.368 mL | 4.7361 mL | 9.4722 mL | 11.8402 mL |
| 10 mM | 0.2368 mL | 1.184 mL | 2.368 mL | 4.7361 mL | 5.9201 mL |
| 50 mM | 0.0474 mL | 0.2368 mL | 0.4736 mL | 0.9472 mL | 1.184 mL |
| 100 mM | 0.0237 mL | 0.1184 mL | 0.2368 mL | 0.4736 mL | 0.592 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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VU 0364439 is a positive allosteric modulator (PAM) of mGlu4 with an EC50 value of 19.8 nM [1] [2] [3].
MGlu4 belongs to metabotropic glutamate receptor (mGluR) group III which contains mGlu4, mGlu6, mGlu7 and mGlu8. MGluRs belong to Class C of G-protein-coupled receptor (GPCR) superfamily. GPCRs modulate postsynaptic effects or the release of glutamate [2].
VU 0364439 exhibited excellent in vitro maximal response and potency relative to another PAM, (−)-PHCCC (a partially selective mGlu4 potentiator, its chemical structure could be found in reference 4). Starting at 30µM, using a 1:3 serial dilutions, VU 0364439 was tested in triplicate. The entire test was performed on one day. Finally, the % (−)-PHCCC value of VU 0364439 was 102.3. The value of % (−)-PHCCC was computed through dividing the maximal response elicited by VU 0364439 by the response of the control PAM, (−)-PHCCC, on the same day. It was also found that the EC50 value of VU 0364439 was 19.8 nM at human mGlu4 [4].
VU 0364439 possessed less than ideal pharmacokinetic properties. The properties of VU 0364439 prevents VU 0364439 itself from being used as an in vivo tool, but VU 0364439 might inform the mGlu4 community with more in vitro tool compounds [4].
References:
[1]. Lucyna Pomierny-Chamioło, Kinga Rup, Bartosz Pomierny, et al. Metabotropic glutamatergic receptors and their ligands in drug addiction. Pharmacology & Therapeutics, 2014, 142:281-305.
[2]. Albert J. Robichaud, Darren W. Engers, Craig W. Lindsley, et al. Recent Progress on the Identification of Metabotropic Glutamate 4 Receptor Ligands and Their Potential Utility as CNS Therapeutics. ACS Chemical Neuroscience, 2011, 2:433-449.
[3]. Colleen M. Niswender, Kari A. Johnson, C. David Weaver, et al. Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. Mol. Pharmacol., 2008, 74(5):1345-1358.
[4]. Darren W. Engers, Patrick R. Gentry, Richard Williams, et al. Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). Bioorg. Med. Chem. Lett., 2010, 20:5175-5178.
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Adicciones. 2016 Oct 6;28(4):189-193.
Editorial of vol 28-4.
[Lessons learned from the evacuation of the VU University Medical Centre after flooding].[Pubmed:28224872]
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.
Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS).[Pubmed:20667732]
Bioorg Med Chem Lett. 2010 Sep 1;20(17):5175-8.
Herein we disclose the synthesis and SAR of a series of 4-(phenylsulfamoyl)phenylacetamide compounds as mGlu(4) positive allosteric modulators (PAMs) that were identified via a functional HTS. An iterative parallel approach to these compounds culminated in the discovery of VU0364439 (11) which represents the most potent (19.8 nM) mGlu(4) PAM reported to date.
