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LX 1606 hippurate is an orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity. Upon administration, LX 1606 hippurate is converted to its active metabolite LP-778902, which binds to and blocks the activity of TPH. This may result in a reduction in peripheral serotonin (5-HT) production and improvement of serotonin-mediated gastrointestinal effects such as severe diarrhea. TPH, the rate-limiting enzyme in serotonin biosynthesis, is overexpressed in carcinoid tumor cells.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | Male C57BL/6 mice and male C57 albino mice. |
| Formulation | 15% cyclodextrin or 0.25% methylcellulose |
| Dosages | ~300 mg/kg |
| Administration | p.o. |
| Molecular Weight | 754.15 |
| Formula | C27H26ClF3N6O3.C9H9NO3 |
| CAS Number | 1137608-69-5 |
| Form | Solid |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] No authors listed. Telotristat
[2] No authors listed. Aust Prescr. Telotristat ethyl for carcinoid syndrome diarrhoea
[3] Mauro Cives, et al. Gastroenteropancreatic Neuroendocrine Tumors
[4] Katherine A Lyseng-Williamson. Telotristat Ethyl: A Review in Carcinoid Syndrome Diarrhoea
| Related Tryptophan Hydroxylase Products |
|---|
| ACT-678689
ACT-678689 (Compound Example 1.53.4) is a tryptophan hydroxylase (TPH) inhibitor with an IC50 of 8 nM. |
| Telotristat
Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC50 of 0.028 μM. |
| LX-1031
LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally. |
| Telotristat ethyl
Telotristat ethyl, also known as LX1606, is an oral serotonin synthesis inhibitor or peripheral tryptophan hydroxylase (TPH) inhibitor. |
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