VU 0364770Positive allosteric modulator at mGlu4 CAS# 61350-00-3 |
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Quality Control & MSDS
3D structure
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| Cas No. | 61350-00-3 | SDF | Download SDF |
| PubChem ID | 836002 | Appearance | Powder |
| Formula | C12H9ClN2O | M.Wt | 232.67 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 100 mg/mL (429.79 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | N-(3-chlorophenyl)pyridine-2-carboxamide | ||
| SMILES | C1=CC=NC(=C1)C(=O)NC2=CC(=CC=C2)Cl | ||
| Standard InChIKey | SUYUTNCKIOLMAJ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C12H9ClN2O/c13-9-4-3-5-10(8-9)15-12(16)11-6-1-2-7-14-11/h1-8H,(H,15,16) | ||
| 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 at mGlu4 receptors (EC50 = 290 nM in mGlu4-expressing HEK 293 cells). Reverses haloperidol-induced catalepsy in rats; prevents attentional deficit and forelimb asymmetry in a rodent model of Parkinson's disease. Exhibits affinity for MAO-B and MAO-A (Ki values are 0.72 μM and 8.5 μM respectively). Brain penetrant. |
VU 0364770 Dilution Calculator
VU 0364770 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 4.2979 mL | 21.4897 mL | 42.9793 mL | 85.9587 mL | 107.4483 mL |
| 5 mM | 0.8596 mL | 4.2979 mL | 8.5959 mL | 17.1917 mL | 21.4897 mL |
| 10 mM | 0.4298 mL | 2.149 mL | 4.2979 mL | 8.5959 mL | 10.7448 mL |
| 50 mM | 0.086 mL | 0.4298 mL | 0.8596 mL | 1.7192 mL | 2.149 mL |
| 100 mM | 0.043 mL | 0.2149 mL | 0.4298 mL | 0.8596 mL | 1.0745 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 0364770 is a positive allosteric modulator(PAM) of mGlu4 with EC50 of 1.1 μM, exhibits insignificant activity at 68 other receptors, including other mGlu subtypes.
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[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.
Why is it (also) so difficult to legislate gambling in Spain? 'Deja vu' of what occurred with alcohol.[Pubmed:27749963]
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Editorial of vol 28-4.
The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease.[Pubmed:22088953]
J Pharmacol Exp Ther. 2012 Feb;340(2):404-21.
Parkinson's disease (PD) is a debilitating neurodegenerative disorder associated with severe motor impairments caused by the loss of dopaminergic innervation of the striatum. Previous studies have demonstrated that positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGlu(4)), including N-phenyl-7-(hydroxyimino) cyclopropa[b]chromen-1a-carboxamide, can produce antiparkinsonian-like effects in preclinical models of PD. However, these early mGlu(4) PAMsexhibited unsuitable physiochemical properties for systemic dosing, requiring intracerebroventricular administration and limiting their broader utility as in vivo tools to further understand the role of mGlu(4) in the modulation of basal ganglia function relevant to PD. In the present study, we describe the pharmacologic characterization of a systemically active mGlu(4) PAM, N-(3-chlorophenyl)picolinamide (VU0364770), in several rodent PD models. VU0364770 showed efficacy alone or when administered in combination with L-DOPA or an adenosine 2A (A2A) receptor antagonist currently in clinical development (preladenant). When administered alone, VU0364770 exhibited efficacy in reversing haloperidol-induced catalepsy, forelimb asymmetry-induced by unilateral 6-hydroxydopamine (6-OHDA) lesions of the median forebrain bundle, and attentional deficits induced by bilateral 6-OHDA nigrostriatal lesions in rats. In addition, VU0364770 enhanced the efficacy of preladenant to reverse haloperidol-induced catalepsy when given in combination. The effects of VU0364770 to reverse forelimb asymmetry were also potentiated when the compound was coadministered with an inactive dose of L-DOPA, suggesting that mGlu(4) PAMs may provide L-DOPA-sparing activity. The present findings provide exciting support for the potential role of selective mGlu(4) PAMs as a novel approach for the symptomatic treatment of PD and a possible augmentation strategy with either L-DOPA or A2A antagonists.
