Telotristat etiprate
Based on 5 publication(s) in Google Scholar
Telotristat etiprate (LX1606 Hippurate) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.
For research use only. We do not sell to patients.
- Purity: 99.89%
- CAS No.: 1137608-69-5
- Formula: C36H35ClF3N7O6
- Molecular Weight:754.15
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Telotristat etiprate
More
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RBL-2H3 | IC50 |
0.4 μM
Compound: 33
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Antiproliferative activity against rat RBL-2H3 cells assessed as inhibition of growth inhibition
Antiproliferative activity against rat RBL-2H3 cells assessed as inhibition of growth inhibition
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[PMID: 36155354] |
Telotristat ethyl (15, 50, 150, 300 mg/kg) depletes 5-HT from the jejunum but not the brain. But Telotristat ethyl (200 mg/kg, p.o.) does not deplete enteric neuronal serotonin (5-HT), or alter constitutive gastrointestinal motility in mice. Telotristat ethyl (200 mg/kg) alleviates the severity of trinitrobenzene sulfonic acid (TNBS)-induced colitis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1137608-69-5
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Appearance Solid
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Molecular Weight 754.15
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Formula C36H35ClF3N7O6
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Color White to off-white
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SMILES
O=C([C@H](CC1=CC=C(C=C1)C2=CC(O[C@H](C3=C(C=C(C=C3)Cl)N4C=CC(C)=N4)C(F)(F)F)=NC(N)=N2)N)OCC.O=C(C5=CC=CC=C5)NCC(O)=O
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Synonyms
LX1606 Hippurate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
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Journal Impact Factor
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Most Recent
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Microb Biotechnol
Protective Effect of Pediococcus pentosaceus Li05 on Constipation via TGR5/TPH1/5-HT Activation. [Abstract]2025 Nov;18(11):e70257. PMID: 41159760 -
Ecotoxicol Environ Saf
Inhaling arsenic aggravates airway hyperreactivity by upregulating PNEC-sourced 5-HT in OVA-induced allergic asthma. [Abstract]2025 Jan 22:290:117764. PMID: 39854863 -
Nutrients
Roseburia hominis Increases Intestinal Melatonin Level by Activating p-CREB-AANAT Pathway. [Abstract]2021 Dec 28;14(1):117. PMID: 35010992 -
Curr Res Microb Sci
Bifidobacterium stercoris KC84 attenuates IBS-D-like symptoms via modulation of serotonin-related pathways and dendritic cell-mediated IFN-β induction. [Abstract]2026 May 10:10:100603. PMID: 42199361 -
mBio
The swine acute diarrhea syndrome coronavirus spike protein promotes syncytial formation via upregulation of cellular cholesterol synthesis. [Abstract]2025 Aug 13;16(8):e0097625. PMID: 40586601
Solvent & Solubility
DMSO : 200 mg/mL (265.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 10 mg/mL (13.26 mM); Clear solution
This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
For studies of the effects of peripheral TPH inhibitors on gut and brain 5-HT concentrations, LP-920540 is formulated in 0.1% Tween 80 in 0.25% methylcellulose and administered to mice once daily via oral gavage at 10 mL/kg for 4 consecutive days. Telotristat ethyl is formulated in 15% cyclodextrin (CaptisolTM, pH 3-4) or 0.25% methylcellulose and given to mice once daily via oral gavage at 10 mL/kg for 4 consecutive days. Whole brain, jejunum and colon (mesentery fat removed, gut lumen opened and blotted dry) are collected, snap frozen, and stored at -80ºC for future. LP-920540, Telotristat ethyl, LP-778914, LP-778920 and vehicle control are also formulated with 0.5% methycellulose at appropriate doses in coded vials. The contents of the coded vials are given by oral gavage in amounts determined by the weights of the recipient mice. After the experiments, results are analyzed.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.3260 mL | 6.6300 mL | 13.2600 mL | 33.1499 mL |
| 5 mM | 0.2652 mL | 1.3260 mL | 2.6520 mL | 6.6300 mL | |
| 10 mM | 0.1326 mL | 0.6630 mL | 1.3260 mL | 3.3150 mL | |
| 15 mM | 0.0884 mL | 0.4420 mL | 0.8840 mL | 2.2100 mL | |
| 20 mM | 0.0663 mL | 0.3315 mL | 0.6630 mL | 1.6575 mL | |
| 25 mM | 0.0530 mL | 0.2652 mL | 0.5304 mL | 1.3260 mL | |
| 30 mM | 0.0442 mL | 0.2210 mL | 0.4420 mL | 1.1050 mL | |
| 40 mM | 0.0331 mL | 0.1657 mL | 0.3315 mL | 0.8287 mL | |
| 50 mM | 0.0265 mL | 0.1326 mL | 0.2652 mL | 0.6630 mL | |
| 60 mM | 0.0221 mL | 0.1105 mL | 0.2210 mL | 0.5525 mL | |
| 80 mM | 0.0166 mL | 0.0829 mL | 0.1657 mL | 0.4144 mL | |
| 100 mM | 0.0133 mL | 0.0663 mL | 0.1326 mL | 0.3315 mL |
Telotristat etiprate Related Classifications
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