ST 1936 oxalateSelective, high affinity 5-HT6 agonist CAS# 1210-81-7 |
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Quality Control & MSDS
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| Cas No. | 1210-81-7 | SDF | Download SDF |
| PubChem ID | 90488934 | Appearance | Powder |
| Formula | C15H19ClN2O4 | M.Wt | 326.78 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO | ||
| Chemical Name | 2-(5-chloro-2-methyl-1H-indol-3-yl)-N,N-dimethylethanamine;oxalic acid | ||
| SMILES | CC1=C(C2=C(N1)C=CC(=C2)Cl)CCN(C)C.C(=O)(C(=O)O)O | ||
| Standard InChIKey | FHSPBPPTDFRVGQ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C13H17ClN2.C2H2O4/c1-9-11(6-7-16(2)3)12-8-10(14)4-5-13(12)15-9;3-1(4)2(5)6/h4-5,8,15H,6-7H2,1-3H3;(H,3,4)(H,5,6) | ||
| 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 | High affinity, selective agonist of 5-HT6 receptors (Ki values are 13, 168, and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors respectively). Displays moderate affinity for human α2 adrenergic receptors (Ki = 300 nM). Shown to increase Ca2+ concentration and phosphorylation of Fyn kinase, and regulate the activation of ERK1/2 in cloned cells. |
ST 1936 oxalate Dilution Calculator
ST 1936 oxalate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.0602 mL | 15.3008 mL | 30.6016 mL | 61.2033 mL | 76.5041 mL |
| 5 mM | 0.612 mL | 3.0602 mL | 6.1203 mL | 12.2407 mL | 15.3008 mL |
| 10 mM | 0.306 mL | 1.5301 mL | 3.0602 mL | 6.1203 mL | 7.6504 mL |
| 50 mM | 0.0612 mL | 0.306 mL | 0.612 mL | 1.2241 mL | 1.5301 mL |
| 100 mM | 0.0306 mL | 0.153 mL | 0.306 mL | 0.612 mL | 0.765 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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ST1936 stimulates cAMP, Ca2+, ERK1/2 and Fyn kinase through a full activation of cloned human 5-HT6 receptors.[Pubmed:21549693]
Eur J Pharmacol. 2011 Jul 1;661(1-3):8-14.
5-HT(6) receptor is one of the most recently cloned serotonin receptors, and it might play important roles in Alzheimer's disease, depression, and learning and memory disorders. Availability of only very few 5-HT(6) receptor agonists, however, does not allow examining their contribution in psychopharmacological processes. Therefore, a new 5-HT(6) receptor agonist, ST1936, was synthesized. ST1936 binds to human 5-HT(6) receptors with good affinity (K(i)=28.8 nM). ST1936 also exhibited some moderate binding affinity for 5HT(2B), 5HT(1A), 5HT(7) receptors and adrenergic alpha receptors. ST1936 behaved as a full 5-HT(6) agonist on cloned cells and was able to increase Ca(2+) concentration, phosphorylation of Fyn kinase, and regulate the activation of ERK1/2 that is a downstream target of Fyn kinase. These effects were completely antagonized by two 5-HT(6) receptor antagonists, SB271046 and SB258585. The other 5-HT(6) receptor agonist, WAY181187 also increased Fyn kinase activity. These results suggest that both ST1936 and WAY181187 mediate 5-HT(6) receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonists.
A microdialysis study of ST1936, a novel 5-HT6 receptor agonist.[Pubmed:21185318]
Neuropharmacology. 2011 Mar;60(4):602-8.
The function of 5-HT6 receptors, one of the last additions to the large family of 5-HT receptors, is largely unknown due to the limited knowledge of their transduction mechanisms, lack of full centrally acting agonists and inconsistencies in the pharmacological and neurochemical effects of the antagonists. Recently, a new full agonist, ST1936, with nanomolar affinity for 5-HT6 receptors, has become available. Here we report the effect of ST1936 (5-10-20 mg/kg/ip) on dialysate DA, NA and 5-HT in the medial prefrontal cortex (PFCX) and in the shell and core of the nucleus accumbens (NAc). Systemic administration of ST1936 dose-dependently increased dialysate DA and NA in the NAc shell and PFCX and to a lesser extent in the NAc core; these effects were prevented by systemic administration of the two 5-HT6 receptor antagonists, SB271046 (10-20 mg/kg/ip) and SB399885 (5 mg/kg/ip). These properties of ST1936 suggest that 5-HT6 receptors control the activity of DA and NA neurons projecting to the NAc and to the PFCX.
