VU 0238429Selective positive allosteric modulator of M5 receptors CAS# 1160247-92-6 |
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| 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. |
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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 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
VU 0238429 Molarity Calculator
| 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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[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.
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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