| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
The primary target of TP003 is the GABA-A receptor, specifically the α3 subunit. It acts as a positive allosteric modulator (PAM), binding to a site on the receptor that is distinct from the GABA binding site. This enhances the effects of GABA, increasing chloride influx and neuronal inhibition. The selective modulation of α3-containing receptors is thought to mediate anxiolytic effects without sedation.
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| ln Vitro |
In vitro, TP003 has been shown to potentiate GABA-induced chloride currents in cells expressing GABA-A receptors containing the α3 subunit. It selectively enhances the activity of α3-containing receptors over other subunits. The compound's effects on receptor function have been demonstrated using electrophysiological techniques.
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| ln Vivo |
In vivo, TP003 has been shown to have anxiolytic effects in animal models of anxiety. It reduces anxiety-like behavior without causing sedation or motor impairment. The compound is administered orally or intraperitoneally in preclinical studies. Its selective modulation of α3-containing receptors is thought to be responsible for its anxiolytic effects.
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| Enzyme Assay |
In vitro enzyme or receptor binding assays for TP003 involve studying its binding to the GABA-A receptor. Radioligand binding assays are performed using membrane preparations from cells expressing GABA-A receptors with different subunit compositions. The compound is incubated with a radiolabeled ligand, and the displacement of the ligand is measured to determine the affinity. Selectivity for α3-containing receptors is assessed.
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| Cell Assay |
In vitro cell-based assays for TP003 are performed using cells expressing GABA-A receptors with different subunit compositions. Cells are treated with the compound, and GABA-induced chloride currents are measured using patch-clamp electrophysiology or using fluorescent dyes to measure chloride flux. The potentiation of GABA-induced currents is used to assess PAM activity.
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| Animal Protocol |
In vivo animal experiments for TP003 are conducted using rodent models of anxiety, such as the elevated plus maze, light-dark box, and open field test. The compound is administered orally or intraperitoneally, and anxiety-like behavior is assessed. The compound's effects on sedation and motor coordination are evaluated using the rotarod test and locomotor activity monitoring.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of TP003 indicate that it is orally active. The compound has a molecular weight of 331.37 and a molecular formula of C19H21N3O3. It is a solid at room temperature. Specific PK parameters, such as half-life and bioavailability, are determined in preclinical studies via LC-MS/MS analysis of plasma samples. The compound is metabolized in the liver and excreted renally.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for TP003 are characteristic of a research compound. As a GABA-A receptor PAM, its safety profile is an important consideration. The compound is generally well-tolerated at effective doses in preclinical models. However, its long-term safety profile requires further evaluation. The compound is for research use only.
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| References | |
| Additional Infomation |
Other information: TP003 is a positive allosteric modulator of the GABA-A receptor, targeting the α3 subunit. It is a research compound used to study the role of GABA-A receptor subtypes in anxiety. Its CAS number is 628690-75-5.
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| Molecular Formula |
C23H16F3N3O
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|---|---|
| Molecular Weight |
407.4
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| Exact Mass |
407.125
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| CAS # |
628690-75-5
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| PubChem CID |
10001434
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| Appearance |
White to off-white solid powder
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| LogP |
5.184
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
667
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SJMMDWXJSSJHOQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H16F3N3O/c1-23(2,30)18-7-8-29-20(12-28-22(29)21(18)26)13-3-6-19(25)17(10-13)16-5-4-15(24)9-14(16)11-27/h3-10,12,30H,1-2H3
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| Chemical Name |
5-fluoro-2-[2-fluoro-5-[8-fluoro-7-(2-hydroxypropan-2-yl)imidazo[1,2-a]pyridin-3-yl]phenyl]benzonitrile
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| Synonyms |
TP-003; TP 003; TP003
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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) |
DMSO : ~100 mg/mL (~245.47 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 | 2.4546 mL | 12.2730 mL | 24.5459 mL | |
| 5 mM | 0.4909 mL | 2.4546 mL | 4.9092 mL | |
| 10 mM | 0.2455 mL | 1.2273 mL | 2.4546 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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