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| ln Vitro |
In PC12 cells (primary screening), TCS 2210 induced neurite outgrowth and increased neuronal markers β-III tubulin and neuron-specific enolase (NSE). In rat bone marrow MSCs, treatment with 20 μM TCS 2210 for 2 days caused significant morphological changes (neuronal-like phenotype) and increased β-III tubulin expression (Western blot and immunocytochemistry) without cytotoxicity. Nissl staining showed that >95% of MSCs converted to a neuronal phenotype after 48 h at 20 μM. TCS 2210 time-dependently increased β-III tubulin and NSE expression. Glial fibrillary acidic protein (GFAP, an astroglial marker) was not detected. Whole-cell patch clamp recordings showed that TCS 2210-treated MSCs exhibited outward K+ currents when voltage steps from -30 to 90 mV were applied, indicating neural electrophysiological properties; untreated MSCs showed no detectable outward current. Gene expression profiling by DNA microarray and quantitative PCR revealed that TCS 2210 dose-dependently increased cholinergic neuron receptor genes (Chrna2, Chrnb2, Chrma) and neuron-specific genes Fbxo2 and Sizn1. In FLIPR membrane potential assays, addition of acetylcholine (10 μM) to TCS 2210-treated MSCs induced a change in membrane potential, confirming cholinergic neuron properties [1].
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| Cell Assay |
Rat MSCs were isolated from bone marrow and characterized. Cells were treated with 20 μM TCS 2210 for 2 days. Immunocytochemistry: cells stained with anti-β-III tubulin antibody and DAPI. Western blot: protein lysates probed with antibodies against β-III tubulin, NSE, and GFAP. Nissl staining: used for neuron detection; differentiation efficiency estimated by cell counting. Whole-cell patch clamp: membrane currents recorded; K+ currents assessed by applying voltage pulses from -30 to 90 mV; data analyzed with pClamp 8.1. Quantitative PCR: mRNA levels of Chrna2, Chrnb2, Fbxo2, Sizn1 determined. FLIPR membrane potential assay: MSCs treated with 20 μM TCS 2210 for 48 h, then 10 μM acetylcholine added, and membrane potential changes detected using a FLIPR assay kit and Flex station software [1].
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| Toxicity/Toxicokinetics |
No cytotoxicity was observed in MSCs treated with 20 μM TCS 2210 for 2 days as determined by cell viability assessment (Figure S3 in Supporting Information) [1].
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| References | |
| Additional Infomation |
TCS 2210 (compound 1) was identified as a novel small molecule that induces neuronal differentiation from mesenchymal stem cells. It is the first reported small molecule that can direct MSCs to differentiate into neurons with demonstrated electrophysiological properties (K+ currents) and cholinergic neuron characteristics (acetylcholine response). It shows no cytotoxicity and is more effective in MSCs than NGF or neuropathiazole. This compound has potential as a tool for studying cell fate determination and for cell therapy applications in neurodegenerative diseases such as Parkinson's and Alzheimer's diseases [1].
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| Molecular Formula |
C18H17N3O3
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|---|---|
| Molecular Weight |
323.352
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| Exact Mass |
323.127
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| Elemental Analysis |
C, 66.86; H, 5.30; N, 13.00; O, 14.84
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| CAS # |
1201916-31-5
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| PubChem CID |
44607172
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.792
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
24
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| Complexity |
500
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ONC(C1=CC=2N=C(CCCC3=CC=CC=C3)C(NC2C=C1)=O)=O
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| InChi Key |
ZOFZKGFBKISZRI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H17N3O3/c22-17(21-24)13-9-10-14-16(11-13)19-15(18(23)20-14)8-4-7-12-5-2-1-3-6-12/h1-3,5-6,9-11,24H,4,7-8H2,(H,20,23)(H,21,22)
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| Chemical Name |
N-hydroxy-2-oxo-3-(3-phenylpropyl)-1H-quinoxaline-6-carboxamide
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| Synonyms |
TCS 2210; TCS-2210; TCS2210
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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 | 3.0926 mL | 15.4631 mL | 30.9262 mL | |
| 5 mM | 0.6185 mL | 3.0926 mL | 6.1852 mL | |
| 10 mM | 0.3093 mL | 1.5463 mL | 3.0926 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.
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