| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
TPH2 agonist-1 (compound 20e) dose-dependently inhibited abnormal electrophysiological activity in iPSC-derived neurons of SMEI patients. At a concentration of 1 μM, it significantly reduced mean firing rate and burst percentage; while at concentrations of 10 μM and 50 μM, it further reduced network burst frequency and duration[1]. Treatment of wild-type (WT) and scn1lab KO zebrafish larvae with TPH2 agonist-1 (5 μM; 4 h) increased serotonin (5-HT) and γ-aminobutyric acid (GABA) levels and restored 5-HT immunoreactivity in the hypothalamus of KO larvae[1].
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| ln Vivo |
TPH2 agonist-1 (compound 20e) showed brain-plasma ratios (B/P) of 4.36, 1.75, and 0.43 in mouse models, adult zebrafish models, and human blood-brain barrier (BBB) systems, respectively [1]. TPH2 agonist-1 (5 mg/kg; administered by gavage; single dose; heat-induced 30 minutes after administration) significantly reduced the severity of seizures in SCN1A+/- mice, prolonged the latency of the first seizure, increased the seizure threshold temperature, and inhibited hyperactivity, without affecting the behavior of wild-type mice [1]. TPH2 agonist-1 (2.5 μM, 5 μM; water exposure; single exposure; recording 30 minutes after exposure) dose-dependently reduced epileptic-like movements in scn1lab KO zebrafish larvae, with a reduction of 41.58% at 2.5 μM and 16.3% at 5 μM. It did not affect the normal movement of wild-type zebrafish and restored the blue preference of KO larvae [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: VERO, HFL-1, L929, NIH3T3, CHO-K1 Test concentrations: 0.01 μM, 0.1 μM, 1 μM, 10 μM, 100 μM Incubation Duration: 24 hours Experimental Results: The viability of various mammalian cell lines was not affected. The IC50 values of all tested cell lines were greater than 100 μM as determined by WST analysis. |
| Animal Protocol |
Animal/Disease Models:13-15 week old male and female 129S-Scn1atm1Kea/Mmjax heterozygous mice (SCN1A+/-) and their wild-type littermates + SMEI model [1]
Doses: 5 mg/kg Route of Administration: Gavage; Frequency: Single dose; 30 minutes before heat induction Experimental Results: Significantly reduced the severity of seizures in SCN1A+/- mice, with a 52% reduction in Racine score compared to the vector control group, prolonged the latency of the first seizure, and increased the seizure threshold temperature. In addition, it also suppressed the hyperactivity of SCN1A+/- mice by reducing the total movement distance and average speed without affecting the movement behavior of wild-type mice. |
| References |
| Molecular Formula |
C15H8CLF4N3O2
|
|---|---|
| Molecular Weight |
373.69
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
FC(C=C1)=CC(Cl)=C1CN2C(OC(C3=CC(C(F)(F)F)=NC=C3)=N2)=O
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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)
|
| 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 | 2.6760 mL | 13.3801 mL | 26.7601 mL | |
| 5 mM | 0.5352 mL | 2.6760 mL | 5.3520 mL | |
| 10 mM | 0.2676 mL | 1.3380 mL | 2.6760 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
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