product name Telotristat
Description: Telotristat is the active metabolite of LX1606(Telotristat etiprate), which is an orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity. Telotristat has activity in controlling diarrhea associated with carcinoid syndrome. Telotristat acts by inhibiting the enzyme tryptophan hydoxylase (TPH) and reduces serotonin production both inside and outside the GI tract without affecting brain serotonin levels.
References: Gut. 2014 Jun;63(6):928-37.
546.93
Formula
C25H22ClF3N6O3
CAS No.
1033805-28-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 10 mM
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
LP778902; LP 778902; LP-778902
other peoduct :
| In Vitro |
In vitro activity: Telotristat reduced 5-HT significantly in the gut and blood but not in the brain. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | LX1606 (LX 1606, LX-1606) is useful for Neurological Diseas [1]. LX1606 were given orally to mice. LX1606 reduced 5-HT significantly in the gut and blood but not in the brain. oral LX1032 reduced the severity of TNBS-induced colitis; the expression of 24% of 84 genes encoding inflammation-related cytokines and chemokines was lowered at least fourfold and the reduced expression of 17% was statistically significant [1]. Treatment with LX1606 showed a strong positive effect in ameliorating TNBS-induced IBD in mice as assessed by various parameters of disease development. These preclinical data demonstrate that inhibition of TPH activity by LX1606 may provide a new approach for the treatment of IBD and its serotonin-mediated symptoms |
| Animal model | Male C57BL/6 mice and male C57 albino mice. |
| Formulation & Dosage | Dissolved in 15% cyclodextrin or 0.25% methylcellulose; 300 mg/kg; p.o. |
| References | Gut. 2014 Jun;63(6):928-37. |
