VU 0238429

Selective positive allosteric modulator of M5 receptors CAS# 1160247-92-6

VU 0238429

Catalog No. BCC7729----Order now to get a substantial discount!

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VU 0238429: 5mg $92 In Stock
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Chemical structure

VU 0238429

3D structure

Chemical Properties of VU 0238429

Cas No. 1160247-92-6 SDF Download SDF
PubChem ID 42633508 Appearance Powder
Formula C17H12F3NO4 M.Wt 351.28
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 150 mg/mL (427.01 mM)
H2O : < 0.1 mg/mL (insoluble)
*"≥" means soluble, but saturation unknown.
Chemical Name 1-[(4-methoxyphenyl)methyl]-5-(trifluoromethoxy)indole-2,3-dione
SMILES COC1=CC=C(C=C1)CN2C3=C(C=C(C=C3)OC(F)(F)F)C(=O)C2=O
Standard InChIKey CKLGZXFOLMHCMC-UHFFFAOYSA-N
Standard InChI InChI=1S/C17H12F3NO4/c1-24-11-4-2-10(3-5-11)9-21-14-7-6-12(25-17(18,19)20)8-13(14)15(22)16(21)23/h2-8H,9H2,1H3
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 VU 0238429

DescriptionSelective positive allosteric modulator of M5 receptors (EC50 values are 1.16, >30 and >30 μM at M5, M1 and M3 receptors respectively). Displays no activity at M2 and M4 receptors.

VU 0238429 Dilution Calculator

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VU 0238429 Molarity Calculator

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Preparing Stock Solutions of VU 0238429

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.8467 mL 14.2337 mL 28.4673 mL 56.9346 mL 71.1683 mL
5 mM 0.5693 mL 2.8467 mL 5.6935 mL 11.3869 mL 14.2337 mL
10 mM 0.2847 mL 1.4234 mL 2.8467 mL 5.6935 mL 7.1168 mL
50 mM 0.0569 mL 0.2847 mL 0.5693 mL 1.1387 mL 1.4234 mL
100 mM 0.0285 mL 0.1423 mL 0.2847 mL 0.5693 mL 0.7117 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 VU 0238429

[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.

Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins.[Pubmed:19438238]

J Med Chem. 2009 Jun 11;52(11):3445-8.

This report describes the discovery and initial characterization of the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5). Functional HTS, identified VU0119498, which displayed micromolar potencies for potentiation of acetylcholine at M1, M3, and M5 receptors in cell-based Ca(2+) mobilization assays. Subsequent optimization led to the discovery of VU0238429, which possessed an EC(50) of approximately 1.16 microM at M5 with >30-fold selectivity versus M1 and M3, with no M2 or M4 potentiator activity.

Description

VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.

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