| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
TCS-1105 targets GABAA benzodiazepine receptors (BZR). It acts as an agonist at α2 subunit-containing GABAA receptors and an antagonist at α1 subunit-containing GABAA receptors. The compound has Ki values of 118 nM for the α2 receptor and 245 nM for the α1 receptor. This functional selectivity is responsible for its anxiolytic effects without sedation.
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| ln Vitro |
In vitro, TCS-1105 acts as a ligand for GABAA benzodiazepine receptors. It shows binding affinity (Ki) of 118 nM for α2 receptors and 245 nM for α1 receptors. It also blocks Sema3A-induced axon growth cone collapse. The compound's in vitro activity is characterized by its differential modulation of GABAA receptor subtypes.
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| ln Vivo |
In vivo, TCS-1105 reduces anxiety-like behavior in mice. It also enhances aggressive behavior and social dominance. Importantly, it is an anxiolytic agent that lacks sedative activity, which is a significant advantage over non-selective benzodiazepines. Its effects are mediated through its action at α2 and α1 GABAA receptors.
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| Enzyme Assay |
In vitro receptor binding assays for TCS-1105 typically involve competitive binding studies using membranes from cells expressing specific GABAA receptor subtypes (α1, α2, etc.). Radiolabeled benzodiazepine ligands (e.g., 3H-flumazenil) are used, and the compound is tested at various concentrations to determine its affinity (Ki values) for the different subtypes.
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| Cell Assay |
In vitro cellular assays for TCS-1105 are used to study its functional effects on GABAA receptors. Electrophysiological techniques, such as patch-clamp recordings, can be performed on cells expressing specific GABAA receptor subtypes to measure the chloride currents elicited by GABA in the presence and absence of the compound. This helps to confirm its agonist or antagonist activity at different receptor subtypes.
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| Animal Protocol |
In vivo animal studies with TCS-1105 are typically conducted in mouse models to assess its behavioral effects. The compound is administered systemically, and tests such as the elevated plus maze, open field test, or light-dark box are used to evaluate anxiety-like behavior. Other behavioral tests may be used to assess aggression and social dominance.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of TCS-1105 are not extensively reported in the available literature. It has a molecular weight of 296.3 and is typically stored at room temperature. Specific parameters such as oral bioavailability, half-life, and tissue distribution are not detailed.
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| Toxicity/Toxicokinetics |
The toxicity profile of TCS-1105 is not extensively reported. As a research compound, it is for research use only and not for human therapeutic use. Its lack of sedative activity suggests a potentially improved safety profile compared to non-selective benzodiazepines, but formal toxicity studies would be required for therapeutic development.
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| References |
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| Additional Infomation |
TCS-1105 is a functionally selective GABAA benzodiazepine receptor ligand that acts as an agonist at α2 receptors and an antagonist at α1 receptors. It is an anxiolytic agent that lacks sedative activity. The compound reduces anxiety-like behavior and enhances aggression and social dominance in mice. It is available for research purposes only.
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| Molecular Formula |
C17H13FN2O2
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|---|---|
| Molecular Weight |
296.295727491379
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| Exact Mass |
296.096
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| CAS # |
185391-33-7
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| PubChem CID |
2986030
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| Appearance |
White to off-white solid powder
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| LogP |
3.197
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
421
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VWCCHJFFYCGXFL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H13FN2O2/c18-12-7-5-11(6-8-12)9-20-17(22)16(21)14-10-19-15-4-2-1-3-13(14)15/h1-8,10,19H,9H2,(H,20,22)
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| Chemical Name |
N-[(4-fluorophenyl)methyl]-2-(1H-indol-3-yl)-2-oxoacetamide
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~125 mg/mL (~421.87 mM)
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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 | 3.3750 mL | 16.8748 mL | 33.7496 mL | |
| 5 mM | 0.6750 mL | 3.3750 mL | 6.7499 mL | |
| 10 mM | 0.3375 mL | 1.6875 mL | 3.3750 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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