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Telotristat
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Catalog No. T21506Cas No. 1033805-28-5
Telotristat is the active metabolite of LX1606(Telotristat etiprate), which is an orally bioavailable tryptophan hydroxylase (TPH) inhibitor and shows potential antiserotonergic activity.
Telotristat
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Purity: 99.70%
Catalog No. T21506Cas No. 1033805-28-5
Telotristat is the active metabolite of LX1606(Telotristat etiprate), which is an orally bioavailable tryptophan hydroxylase (TPH) inhibitor and shows potential antiserotonergic activity.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $41 | In Stock | In Stock | |
| 10 mg | $59 | In Stock | In Stock | |
| 25 mg | $128 | In Stock | In Stock | |
| 50 mg | $208 | In Stock | In Stock | |
| 100 mg | $337 | In Stock | In Stock | |
| 200 mg | $470 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $50 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:99.70%
Appearance:Solid
Color:White
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Product Introduction
Telotristat AI Summary
Telotristat is a multifunctional molecule known primarily for its inhibition of TPH1 with an IC50 value of 16.0 nM, and it also demonstrates substantial inhibitory activity against TPH2, with an IC50 value of 710.0 nM. This compound affects the serotonin biosynthesis pathway by reducing the formation of 5-HTP. Additionally, Telotristat has been evaluated for antiviral activity against SARS-CoV-2, displaying potential off-disease activity with a hit score of -0.05214 in HRCE cells, and an IC50 value greater than 20,000 nM for preventing virus-induced cytotoxicity in VERO-6 cells. Beyond these activities, it shows a broad spectrum of bioactivities, including binding affinity to numerous receptors (e.g., DRD1, DRD2, DRD3, ESR1, SLC6A3) and exhibiting agonist activity at receptors like HRH2, HTR2B, ADRA2A. It also inhibits enzymes such as PTGS2, PTGS1, and PDE4A. This extensive profile indicates Telotristat as a potential modulator across multiple pathways and targets..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Telotristat is the active metabolite of LX1606(Telotristat etiprate), which is an orally bioavailable tryptophan hydroxylase (TPH) inhibitor and shows potential antiserotonergic activity. |
| Targets&IC50 | TPH:0.028 μM |
| Molecular Weight | 546.93 |
| Formula | C25H22ClF3N6O3 |
| Cas No. | 1033805-28-5 |
| Smiles | Cc1ccn(n1)-c1cc(Cl)ccc1[C@@H](Oc1cc(nc(N)n1)-c1ccc(C[C@H](N)C(O)=O)cc1)C(F)(F)F |
| Relative Density. | 1.50 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (91.42 mM), Sonication is recommended.  Ethanol: insoluble H2O: insoluble | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.66 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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