SGS 518 oxalateSelective 5-HT6 antagonist CAS# 445441-27-0 |
2D Structure
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
Cas No. | 445441-27-0 | SDF | Download SDF |
PubChem ID | 71433764 | Appearance | Powder |
Formula | C23H24F2N2O6S | M.Wt | 494.5 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Synonyms | LY 483518 | ||
Solubility | Soluble to 100 mM in DMSO | ||
Chemical Name | [1-methyl-3-(1-methylpiperidin-4-yl)indol-5-yl] 2,6-difluorobenzenesulfonate;oxaldehydic acid | ||
SMILES | CN1CCC(CC1)C2=CN(C3=C2C=C(C=C3)OS(=O)(=O)C4=C(C=CC=C4F)F)C.C(=O)C(=O)O | ||
Standard InChIKey | QFZRGMRDHHDVBY-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C21H22F2N2O3S.C2H2O3/c1-24-10-8-14(9-11-24)17-13-25(2)20-7-6-15(12-16(17)20)28-29(26,27)21-18(22)4-3-5-19(21)23;3-1-2(4)5/h3-7,12-14H,8-11H2,1-2H3;1H,(H,4,5) | ||
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 antagonist of the 5-HT6 subtype of the serotonin receptor. Useful for the treatment of cognitive impairment that is associated with schizophrenia and Alzheimer's disease. |
SGS 518 oxalate Dilution Calculator
SGS 518 oxalate Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.0222 mL | 10.1112 mL | 20.2224 mL | 40.4449 mL | 50.5561 mL |
5 mM | 0.4044 mL | 2.0222 mL | 4.0445 mL | 8.089 mL | 10.1112 mL |
10 mM | 0.2022 mL | 1.0111 mL | 2.0222 mL | 4.0445 mL | 5.0556 mL |
50 mM | 0.0404 mL | 0.2022 mL | 0.4044 mL | 0.8089 mL | 1.0111 mL |
100 mM | 0.0202 mL | 0.1011 mL | 0.2022 mL | 0.4044 mL | 0.5056 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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New serotonin 5-HT(6) ligands from common feature pharmacophore hypotheses.[Pubmed:18044950]
J Chem Inf Model. 2008 Jan;48(1):197-206.
Serotonin 5-HT6 receptor antagonists are thought to play an important role in the treatment of psychiatry, Alzheimer's disease, and probably obesity. To find novel and potent 5-HT6 antagonists and to provide a new idea for drug design, we used a ligand-based pharmacophore to perform the virtual screening of a commercially available database. A three-dimensional common feature pharmacophore model was developed by using the HipHop program provided in Catalyst software and was used as a query for screening the database. A recursive partitioning (RP) model which can separate active and inactive compounds was used as a filtering system. Finally a sequential virtual screening procedure (SQSP) was conducted, wherein both the common feature pharmacophore and the RP model were used in succession to improve the results. Some of the hits were selected based on druglikeness, ADME properties, structural diversity, and synthetic accessibility for real biological evaluation. The best hit compound showed a significant IC50 value of 9.6 nM and can be used as a lead for further drug development.
Efficacy of selective 5-HT6 receptor ligands determined by monitoring 5-HT6 receptor-mediated cAMP signaling pathways.[Pubmed:16865095]
Br J Pharmacol. 2006 Aug;148(8):1133-43.
1. Two novel selective 5-HT6 receptor ligands E-6801 (6-chloro-N-(3-(2-(dimethylamino)ethyl)-1H-indol-5-yl)imidazo[2,1-b]thiazole-5-su lfonamide) and E-6837 (5-chloro-N-(3-(2-(dimethylamino)ethyl)-1H-indol-5-yl)naphthalene-2-sulfonamide) were investigated and compared to the putative 5-HT6 receptor antagonists SB-271046 (5-chloro-N-(4-methoxy-3-(piperazin-1-yl)phenyl)-3-methylbenzo[b]thiophene-2-sulf onamide) and Ro 04-06790 (N-(2,6-bis(methylamino)pyrimidin-4-yl)-4-aminobenzenesulfonamide) using a cAMP-mediated pathway. 2. Forskolin stimulation, to increase the magnitude of agonist cAMP responses, and site-directed mutagenesis of the 5-HT6 receptor, in order to yield constitutively active receptor, were applied. 3. 5-HT (E(max), % over basal: 200), E-6801 (120) and E-6837 (23) induced cAMP formation at the rat 5-HT6 receptor. In the copresence of forskolin, cAMP responses were more potent and enhanced to 294 (5-HT, % over forskolin), 250 (E-6801) and 207 (E-6837), respectively. 5-HT-mediated cAMP formation was dose-dependently blocked by SB-271046 (pA(2): 8.76+/-0.22) and Ro 04-6790 (pA(2): 7.89+/-0.10) and not affected by the copresence of forskolin. Both E-6801 and E-6837 yielded partial antagonism of the 5-HT response in the absence of forskolin, whereas antagonism was either completely absent (E-6801) or attenuated (E-6837) in the copresence of forskolin. Intrinsic activity of these 5-HT6 receptor ligands at a constitutively active human S267K 5-HT6 receptor in Cos-7 cells indicated similar efficacy (E(max), % over basal) for 5-HT (97), E-6801 (91) and E-6837 (100), while Ro 04-6790 (-33) and SB-271046 (-39) were equi-efficacious inverse agonists. 4. The use of either forskolin or a constitutively active S267K 5-HT6 receptor enhances the resolution for monitoring the efficacy of 5-HT6 receptor ligands. E-6801 and E-6837 are potent partial agonists at the 5-HT6 receptor. Ro 04-6790 and SB-271046 appear to act as inverse agonists/antagonists.