VU 0365114Positive allosteric modulator of M5 receptors CAS# 1208222-39-2 |
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| Cas No. | 1208222-39-2 | SDF | Download SDF |
| PubChem ID | 45281794 | Appearance | Powder |
| Formula | C22H14F3NO3 | M.Wt | 397.35 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 77.5 mg/mL (195.04 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 1-[(4-phenylphenyl)methyl]-5-(trifluoromethoxy)indole-2,3-dione | ||
| SMILES | C1=CC=C(C=C1)C2=CC=C(C=C2)CN3C4=C(C=C(C=C4)OC(F)(F)F)C(=O)C3=O | ||
| Standard InChIKey | SPBGRXOPAXZSER-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C22H14F3NO3/c23-22(24,25)29-17-10-11-19-18(12-17)20(27)21(28)26(19)13-14-6-8-16(9-7-14)15-4-2-1-3-5-15/h1-12H,13H2 | ||
| 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 (EC50 values are 2.7 μM for human M5, and >30 μM for M1, M2, M3 and M4 receptors). |
VU 0365114 Dilution Calculator
VU 0365114 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.5167 mL | 12.5834 mL | 25.1667 mL | 50.3335 mL | 62.9168 mL |
| 5 mM | 0.5033 mL | 2.5167 mL | 5.0333 mL | 10.0667 mL | 12.5834 mL |
| 10 mM | 0.2517 mL | 1.2583 mL | 2.5167 mL | 5.0333 mL | 6.2917 mL |
| 50 mM | 0.0503 mL | 0.2517 mL | 0.5033 mL | 1.0067 mL | 1.2583 mL |
| 100 mM | 0.0252 mL | 0.1258 mL | 0.2517 mL | 0.5033 mL | 0.6292 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.
Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.[Pubmed:20004578]
Bioorg Med Chem Lett. 2010 Jan 15;20(2):558-62.
This Letter describes a chemical lead optimization campaign directed at VU0238429, the first M(5)-preferring positive allosteric modulator (PAM), discovered through analog work around VU0119498, a pan G(q) mAChR M(1), M(3), M(5) PAM. An iterative library synthesis approach delivered the first selective M(5) PAM (no activity at M(1)-M(4) @ 30microM), and an important tool compound to study the role of M(5) in the CNS.
Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators.[Pubmed:20801651]
Bioorg Med Chem Lett. 2010 Oct 1;20(19):5617-22.
This Letter describes a chemical lead optimization campaign directed at VU0238429, the first M(5)-preferring positive allosteric modulator (PAM), discovered through analog work around VU0119498, a pan G(q) mAChR M(1), M(3), M(5) PAM. An iterative parallel synthesis approach was employed to incorporate basic heterocycles to improve physiochemical properties.
VU 0365114 is a mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM.
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