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100mg | ||
250mg | ||
500mg |
ln Vitro |
While tested on a broad cross-reactivity panel including G-proteins, ST1936 Oxalate also demonstrated resistance to 5-HT2B, 5-HT1A, 5-HT7 Affinity of receptors, and alpha-adrenergic receptors, it appears to be somewhat selective for the 5-HT6 receptor. transporters, enzymes, ion channel binding sites, and coupled receptors [1]. In clonal cells, ST1936 oxalate functions as a complete 5-HT6 agonist by elevating Ca2+ levels, phosphorylating Fyn kinase, and controlling the activation of Fyn kinase's downstream target, ERK1/2 [2]. With an IC50 of 1.3 μM, ST1936 oxalate lowers the frequency of spontaneous excitatory postsynaptic currents [3].
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ln Vivo |
Extracellular dopamine (DA) and NA levels in the prefrontal cortex (PFCX) are raised in a dose-dependent manner by ST1936 (5, 10, 20 mg/kg; i.p.) oxalate [2]. Oxalate raises the levels of extracellular DA and NA in the nucleus accumbens (NAc) core (ST1936; 5, 10, 20 mg/kg; i.p.). Higher doses raised dialysate DA and NA (201% and 231%, respectively), while the 10 mg/kg dose increased dialysate DA (peak: 179%). There was no difference at 5 mg/kg [2].
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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. |
Molecular Formula |
C₁₅H₁₉CLN₂O₄
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Molecular Weight |
326.78
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CAS # |
1782228-83-4
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Related CAS # |
ST1936;1210-81-7
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
ClC1C([H])=C([H])C2=C(C=1[H])C(=C(C([H])([H])[H])N2[H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H].O([H])C(C(=O)O[H])=O
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Synonyms |
ST1936 oxalate; ST1936 oxalate
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HS Tariff Code |
2934.99.9001
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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)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.0602 mL | 15.3008 mL | 30.6016 mL | |
5 mM | 0.6120 mL | 3.0602 mL | 6.1203 mL | |
10 mM | 0.3060 mL | 1.5301 mL | 3.0602 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.