| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
| Targets |
5-HT6 Receptor 13 nM (Ki) 5-HT7 Receptor 168 nM (Ki) 5-HT2B Receptor 245 nM (Ki) α1-adrenergic receptor 390 nM (Ki, rat) α2-adrenergic receptor 300 nM (Ki, rat) α2-adrenergic receptor 300 nM (Ki, human)
ST1936 targets the serotonin 5-HT6 receptor with high selectivity. It is a selective agonist with a Ki of 13 nM for human 5-HT6 receptors. It demonstrates notable selectivity across related serotonin receptors, with Ki values of 168 nM for 5-HT7 and 245 nM for 5-HT2B. It also shows moderate affinity for α2-adrenergic receptors with a Ki of 300 nM. The 5-HT6 receptor plays a crucial role in various neurobiological processes, including neurotransmitter release and neural regeneration. |
|---|---|
| ln Vitro |
ST1936 was tested in a broad crossreactivity panel that included G-protein-coupled receptors, ion channel binding sites, transporters, enzymes, and 5-HT6 receptors. It has demonstrated affinity for 5-HT2B, 5-HT1A, 5-HT7, and α-adrenergic receptors, but it appears to be relatively selective for 5-HT6 receptors[1]. In cloned cells, ST1936 acts as a complete 5-HT6 agonist and can raise Ca2+ levels, phosphorylate Fyn kinase, and control the activation of ERK1/2, which is Fyn kinase's downstream target[2]. With an IC50 of 1.3 μM, ST1936 lowers the frequency of spontaneous excitatory postsynaptic currents[3].
In vitro, ST1936 acts as a selective 5-HT6 receptor agonist. It fully activates cloned human 5-HT6 receptors to stimulate cAMP, Ca2+, ERK1/2, and Fyn kinase. The compound shows Ki values of 13 nM for human 5-HT6, 168 nM for 5-HT7, and 245 nM for 5-HT2B receptors. Standard in vitro assays include receptor binding studies using radiolabeled ligands, cAMP accumulation assays, calcium mobilization assays using fluorescent indicators, and Western blot analysis for ERK1/2 and Fyn kinase activation. |
| ln Vivo |
In the prefrontal cortex (PFCX), ST1936 (5, 10, 20 mg/kg; ip) raises extracellular dopamine (DA) and NA levels in a dose-dependent manner[4]. The nucleus accumbens (NAc) core's extracellular DA and NA levels are raised by ST1936 (5, 10, 20 mg/kg; ip). Dialysate DA (peak: 179%) is increased by doses of 10 mg/kg, but dialysate NA (231% and 201%, respectively) is increased by greater doses. Five milligrams per kilogram has no effect[4].
In vivo, ST1936 is used as a research tool to study 5-HT6 receptor function and its role in neurobiological processes. As a 5-HT6 receptor agonist, it would be expected to modulate neurotransmitter release and neural regeneration. The compound has been studied for its potential in cognitive enhancement and neuropsychiatric disorders. However, comprehensive in vivo efficacy data from published literature are limited. The compound is primarily used as a research tool rather than for therapeutic applications. |
| Enzyme Assay |
For non-cell-based receptor binding assays, ST1936 can be evaluated using membrane preparations from cells expressing human 5-HT6, 5-HT7, or 5-HT2B receptors. Radioligand binding displacement experiments are performed using suitable radiolabeled ligands such as [3H]-LSD for 5-HT6 or [3H]-5-HT for other serotonin receptors. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand at room temperature for 60-90 minutes. Bound radioligand is separated from free by rapid filtration through glass fiber filters. Non-specific binding is determined in the presence of excess unlabeled ligand. Ki values are calculated from displacement curves using nonlinear regression analysis.
|
| Cell Assay |
For in vitro cellular assays, cells expressing human 5-HT6 receptors are cultured in appropriate media. For functional assays, cAMP accumulation is measured as 5-HT6 receptors are Gs-coupled. Cells are treated with various concentrations of ST1936, and cAMP levels are measured using ELISA or HTRF-based detection. For calcium mobilization assays, cells are loaded with fluorescent calcium indicators and treated with the compound. For ERK1/2 and Fyn kinase activation assays, cells are treated with the compound and protein phosphorylation is assessed by Western blot using phospho-specific antibodies. EC50 values are calculated from dose-response curves.
|
| Animal Protocol |
For in vivo animal studies, ST1936 can be administered to rodents via intraperitoneal injection. In models of cognitive function, memory and learning tests such as the Morris water maze or novel object recognition are performed following compound administration. In models of neuropsychiatric disorders, behavioral tests are conducted. Dosing regimens vary depending on the specific model and desired exposure levels. Blood and tissue samples may be collected for pharmacokinetic analysis.
|
| ADME/Pharmacokinetics |
ST1936 has a molecular weight of 253.30 and a molecular formula of C15H15N3O. It is a selective 5-HT6 receptor agonist. The compound is supplied as a research-grade compound. It is soluble in DMSO and can be formulated for both in vitro and in vivo administration. It should be stored at -20°C for long-term stability. It is for research use only and is not intended for human consumption.
|
| Toxicity/Toxicokinetics |
The toxicity profile of ST1936 has not been extensively reported. As a 5-HT6 receptor agonist, potential adverse effects may include modulation of serotonergic signaling, which could affect cognition, mood, and neurotransmitter release. The compound is for research use only and is not intended for human consumption. Standard toxicological evaluation would include acute and repeated-dose toxicity studies, as well as assessment of effects on the central nervous system.
|
| References |
[1]. Borsini F, et al. Effects of ST1936, a selective serotonin-6 agonist, on electrical activity of putative mesencephalic dopaminergic neurons in the rat brain. J Psychopharmacol. 2015 Jul;29(7):802-11.
[2]. Riccioni T, et al. ST1936 stimulates cAMP, Ca2+, ERK1/2 and Fyn kinase through a full activation of cloned human 5-HT6 receptors. Eur J Pharmacol. 2011;661(1-3):8-14. [3]. Tassone A, et al. Activation of 5-HT6 receptors inhibits corticostriatal glutamatergic transmission. Neuropharmacology. 2011;61(4):632-637. [4]. Valentini V, et al. A microdialysis study of ST1936, a novel 5-HT6 receptor agonist. Neuropharmacology. 2011;60(4):602-608. |
| Additional Infomation |
ST1936 (CAS 1210-81-7) is a selective agonist of the 5-HT6 receptor with nanomolar affinity. It exhibits Ki values of 13 nM for human 5-HT6, 168 nM for 5-HT7, and 245 nM for 5-HT2B receptors. It also shows moderate affinity for α2-adrenergic receptors with a Ki of 300 nM. ST1936 activates multiple signaling pathways including cAMP, Ca2+, ERK1/2, and Fyn kinase. It is available for research purposes only.
|
| Molecular Formula |
C13H17CLN2
|
|---|---|
| Molecular Weight |
236.74
|
| Exact Mass |
236.108
|
| CAS # |
1210-81-7
|
| Related CAS # |
ST1936 oxalate;1782228-83-4
|
| PubChem CID |
9921064
|
| Appearance |
White to light yellow solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
377.0±42.0 °C at 760 mmHg
|
| Flash Point |
181.8±27.9 °C
|
| Vapour Pressure |
0.0±0.9 mmHg at 25°C
|
| Index of Refraction |
1.614
|
| LogP |
3.31
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
1
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
16
|
| Complexity |
232
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN(CCC1=C(C)NC2=CC=C(C=C12)Cl)C
|
| InChi Key |
KSYMELKKLOFABL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H17ClN2/c1-9-11(6-7-16(2)3)12-8-10(14)4-5-13(12)15-9/h4-5,8,15H,6-7H2,1-3H3
|
| Chemical Name |
2-(5-chloro-2-methyl-1H-indol-3-yl)-N,N-dimethylethanamine
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 100 mg/mL (422.40 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.56 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2240 mL | 21.1202 mL | 42.2404 mL | |
| 5 mM | 0.8448 mL | 4.2240 mL | 8.4481 mL | |
| 10 mM | 0.4224 mL | 2.1120 mL | 4.2240 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
