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.
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|---|---|
| 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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[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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