SF 11NPY Y2 receptor antagonist CAS# 443292-81-7 |
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Quality Control & MSDS
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Chemical structure
3D structure
Cas No. | 443292-81-7 | SDF | Download SDF |
PubChem ID | 2936384 | Appearance | Powder |
Formula | C27H30N2O2S | M.Wt | 446.6 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | Soluble to 100 mM in DMSO and to 50 mM in ethanol | ||
Chemical Name | N-(4-ethoxyphenyl)-4-[hydroxy(diphenyl)methyl]piperidine-1-carbothioamide | ||
SMILES | CCOC1=CC=C(C=C1)NC(=S)N2CCC(CC2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O | ||
Standard InChIKey | PMEQBGAGFZDWQX-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C27H30N2O2S/c1-2-31-25-15-13-24(14-16-25)28-26(32)29-19-17-23(18-20-29)27(30,21-9-5-3-6-10-21)22-11-7-4-8-12-22/h3-16,23,30H,2,17-20H2,1H3,(H,28,32) | ||
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 | NPY Y2 antagonist (IC50 = 199 nM). Displays no affinity for Y1 receptor at concentrations up to 35 μM. Causes significant lethality in mice. Brain penetrant. |
SF 11 Dilution Calculator
SF 11 Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.2391 mL | 11.1957 mL | 22.3914 mL | 44.7828 mL | 55.9785 mL |
5 mM | 0.4478 mL | 2.2391 mL | 4.4783 mL | 8.9566 mL | 11.1957 mL |
10 mM | 0.2239 mL | 1.1196 mL | 2.2391 mL | 4.4783 mL | 5.5979 mL |
50 mM | 0.0448 mL | 0.2239 mL | 0.4478 mL | 0.8957 mL | 1.1196 mL |
100 mM | 0.0224 mL | 0.112 mL | 0.2239 mL | 0.4478 mL | 0.5598 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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[The Health-Related Quality of Life as Measured with the SF-12v1 in Elderly People Living in Luebeck 2010/11 in Comparison with the German Norm Data in 1994].[Pubmed:25350388]
Gesundheitswesen. 2016 Jan;78(1):49-55.
BACKGROUND: Health-related quality of life (HRQL) is deemed to be a meaningful endpoint when evaluating therapy and prevention interventions. For comparison purposes not only patient data but also representative population samples can serve as reference data. We aim to describe differences between the Luebeck population sample (LBS, year 2010/11) and the German norm population from 1994. Moreover, the influence of diabetes mellitus and hypertension on HRQL is analysed. METHODS: The LBS is a representative sample of 10 000 elderly people living in Luebeck aged 51-80 years, an age group susceptible to chronic diseases. Not only the SF-12v1, but also the item "actual health status in comparison to the last year" of the SF-36 and a list of comorbidities have been applied. Descriptive statistics are given for age, sex and disease groups. A comparison with data from the DNSP going back to 1994 is made using unstandardised data as well as age- and gender-standardised data. RESULTS: 5 835 individuals (response rate 60%) did participate in the survey (48% male, mean age 63.9 years, SD 7.7). PSC and MSC could be computed for 80% of them. Unstandardised values are 44.3+/-10.8 for the PSC and 50.4+/-10.3 for the MSC. Applying standardisation by age and gender, PSC values were comparable between the LBS and DNSP (except for the age group 51-60 years). MSC values were significantly lower in the LBS. The "general health Status" does not significantly differ whereas the "actual health status in comparison to the last year" is significantly lower in the LBS than in the DNSP (p<0.001). CONCLUSIONS: The LBS comprises more individuals than older studies in an age group relevant for chronic diseases. RESULTS hint to a comparable physical HRQL but a worse mental HRQL in the current data set. It remains unclear why persons between 51 and 60 years assess their physical HRQL worse than in the DNSP. A further open question is why the "actual health status in comparison to the last year" is assessed more negatively. Changed context conditions in working and social life may have an influence.
Selective and brain penetrant neuropeptide y y2 receptor antagonists discovered by whole-cell high-throughput screening.[Pubmed:19837904]
Mol Pharmacol. 2010 Jan;77(1):46-57.
The role of neuropeptide Y Y2 receptor (Y2R) in human diseases such as obesity, mood disorders, and alcoholism could be better resolved by the use of small-molecule chemical probes that are substantially different from the currently available Y2R antagonist, N-[(1S)-4-[(aminoiminomethyl)amino]-1-[[[2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazoli din-4-yl)ethyl]amino]carbonyl]butyl]-1-[2-[4-(6,11-dihydro-6-oxo-5H-dibenz[b,e]az epin-11-yl)-1-piperazinyl]-2-oxoethyl]-cyclopentaneacetamide) (BIIE0246). Presented here are five potent, selective, and publicly available Y2R antagonists identified by a high-throughput screening approach. These compounds belong to four chemical scaffolds that are structurally distinct from the peptidomimetic BIIE0246. In functional assays, IC(50) values between 199 and 4400 nM against the Y2R were measured, with no appreciable activity against the related NPY-Y1 receptor (Y1R). Compounds also displaced radiolabeled peptide YY from the Y2R with high affinity (K(i) values between 1.55 and 60 nM) while not displacing the same ligand from the Y1R. In contrast to BIIE0246, Schild analysis with NPY suggests that two of the five compounds behave as competitive antagonists. Profiling against a panel of 40 receptors, ion channels, and transporters found in the central nervous system showed that the five Y2R antagonists demonstrate greater selectivity than BIIE0246. Furthermore, the ability of these antagonists to penetrate the blood-brain barrier makes them better suited for pharmacological studies of Y2R function in both the brain and periphery.