LX1606 Hippurate (Telotristat etiprate) (Synonyms: LX 1032 hippurate, LX 1606 hippurate) |
Catalog No.GC10007
One-Click Copy Product Info
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LX1606 Hippurate (Telotristat etiprate) is an oral, systemically available, small-molecule inhibitor of peripheral serotonin (5-HT) synthesis.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1137608-69-5
Sample solution is provided at 25 µL, 10mM.
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LX1606 Hippurate (Telotristat etiprate) is an oral, systemically available, small-molecule inhibitor of peripheral serotonin (5-HT) synthesis[1]. LX1606 Hippurate inhibits tryptophan hydroxylase, thereby inhibiting the excessive production of peripheral 5-HT in the body and reducing symptoms such as defecation and other gastrointestinal issues[2]. LX1606 Hippurate has been widely used to alleviate rheumatoid arthritis and regulate MAPK signaling pathway[3].
In vitro, LX1606 Hippurate treatment for 72 hours significantly inhibited the proliferation of BON-1, QGP-1 and HROC57 cells after 72 hours, with IC50 values of 20.71μM, 23.71μM, and 11.43μM, respectively[4].
In vivo, LX1606 Hippurate treatment via oral administration at a dose of 300mg/kg/day for 6 days alleviated acute dextran sulfate sodium (DSS)-induced colitis and reduced pro-inflammatory cytokine levels in mice[5].
References:
[1] Gelhorn H L, Kulke M H, O’Dorisio T, et al. Patient-reported symptom experiences in patients with carcinoid syndrome after participation in a study of telotristat etiprate: a qualitative interview approach[J]. Clinical Therapeutics, 2016, 38(4): 759-768.
[2] Kulke M H, O'Dorisio T, Phan A, et al. Telotristat etiprate, a novel serotonin synthesis inhibitor, in patients with carcinoid syndrome and diarrhea not adequately controlled by octreotide[J]. Endocrine-Related Cancer, 2014, 21(5): 705-714.
[3] Zhang L, Lin Y, Xu X, et al. Telotristat Etiprate alleviates rheumatoid arthritis by targeting LGALS3 and affecting MAPK signaling[J]. Intractable & Rare Diseases Research, 2023, 12(1): 45-57.
[4] Molina-Cerrillo J, Sierra-Ramirez A, López-Aceituno J L, et al. A Combination of the Tryptophan Hydroxylase Inhibitor Telotristat with the mTOR Inhibitor Everolimus as an Effective Strategy Against Neuroendocrine Tumors: J. Molina-Cerrillo et al[J]. Drugs in R&D, 2026: 1-13.
[5] Kim J J, Wang H, Terc J D, et al. Blocking peripheral serotonin synthesis by telotristat etiprate (LX1032/LX1606) reduces severity of both chemical-and infection-induced intestinal inflammation[J]. American Journal of Physiology-Gastrointestinal and Liver Physiology, 2015, 309(6): G455-G465.
| Cell experiment [1]: | |
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Cell lines |
BON-1 cells |
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Preparation Method |
BON-1 cells were cultured in RPMI-1640 medium supplemented with 10% fetal bovine serum (FBS), and 1% penicillin-streptomycin at 37°C in 5% CO2/atmosphere. BON-1 cells were seeded onto 96-well microplates (1×104 cells/well) and cultured for 24h. Cells were treated with the different concentrations of LX1606 Hippurate (0, 1, 5, 10, and 100μM) for 72h, cell viability was assessed. |
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Reaction Conditions |
0, 1, 5, 10, and 100μM; 72h |
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Applications |
LX1606 Hippurate treatment decreased the cell viability of BON-1 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6 mice |
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Preparation Method |
C57BL/6 mice (8 weeks old) were kept in sterilized, filter-topped cages under specific pathogen-free conditions and fed autoclaved food. Acute colitis was induced by giving 5% DSS in drinking water for 5 days. Mice received vehicle or LX1606 Hippurate at a dosage of 300mg/kg orally every day starting 1 day prior to administration of 5% DSS and were euthanized on day 5 post-DSS to assess disease severity. |
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Dosage form |
300mg/kg/day; 6 days; p.o. |
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Applications |
LX1606 Hippurate treatment significantly alleviated acute DSS-induced colitis in mice. |
References: [1] Molina-Cerrillo J, Sierra-Ramirez A, López-Aceituno J L, et al. A Combination of the Tryptophan Hydroxylase Inhibitor Telotristat with the mTOR Inhibitor Everolimus as an Effective Strategy Against Neuroendocrine Tumors: J. Molina-Cerrillo et al[J]. Drugs in R&D, 2026: 1-13. [2] Kim J J, Wang H, Terc J D, et al. Blocking peripheral serotonin synthesis by telotristat etiprate (LX1032/LX1606) reduces severity of both chemical-and infection-induced intestinal inflammation[J]. American Journal of Physiology-Gastrointestinal and Liver Physiology, 2015, 309(6): G455-G465. | |
| Cas No. | 1137608-69-5 | SDF | |
| Synonyms | LX 1032 hippurate, LX 1606 hippurate | ||
| Chemical Name | 2-benzamidoacetic acid;ethyl (2S)-2-amino-3-[4-[2-amino-6-[(1R)-1-[4-chloro-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]pyrimidin-4-yl]phenyl]propanoate | ||
| Canonical SMILES | CCOC(=O)C(CC1=CC=C(C=C1)C2=CC(=NC(=N2)N)OC(C3=C(C=C(C=C3)Cl)N4C=CC(=N4)C)C(F)(F)F)N.C1=CC=C(C=C1)C(=O)NCC(=O)O | ||
| Formula | C36H35ClF3N7O6 | M.Wt | 754.17 |
| Solubility | DMF: 50 mg/ml,DMSO: 50 mg/ml,DMSO:PBS(pH 7.2) (1:2): 0.33 mg/ml,Ethanol: 5 mg/ml | Storage | Store at -20°C, protected from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.326 mL | 6.6298 mL | 13.2596 mL |
| 5 mM | 265.2 μL | 1.326 mL | 2.6519 mL |
| 10 mM | 132.6 μL | 663 μL | 1.326 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)