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Telotristat ethyl (LX1606) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.
LX1606 (15, 50, 150, 300 mg/kg, po, qd) reduces serotonin content in the periphery, but not in the brain of the mice. Telotristat ethyl (LX1606) (200 mg/kg po, qd) prevents the increase in blood neutrophil counts that is observed after TNBS challenge, provides significant protection in a mouse model of inflammatory bowel disease. LX1606 (200 mg/kg po, qd) protects the mouse IBD model confirmed by histopathology evaluation.
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| Animal models | mice |
| Formulation | formulated in 15% cyclodextrin (Captisol, pH 3-4) or 0.25% methylcellulose |
| Dosages | 10 mL/kg |
| Administration | oral gavage |
| Molecular Weight | 574.98 |
| Formula | C27H26ClF3N6O3 |
| CAS Number | 1033805-22-9 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Etiprate
Telotristat Etiprate (LX 1606 Hippurate) is an orally bioavailable, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity. |
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