product name Telotristat Etiprate
Description: Telotristat Etiprate (also known as LX 1606 Hippurate or LX1032) is an orally bioavailable, peripheral tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity. Telotristat etiprate has activity in controlling diarrhea associated with carcinoid syndrome. Telotristat Etiprate 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.
754.15
Formula
C27H26ClF3N6O3.C9H9NO3
CAS No.
1137608-69-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (132.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Telotristat Etiprate reduced 5-HT significantly in the gut and blood but not in the brain. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Telotristat Etiprate (300 mg/kg p.o.) significantly reduces 5-HT in the gut and blood, but not brain 5-HT. Telotristat Etiprate (200 mg/kg p.o.) alleviates the severity of trinitrobenzene sulfonic acid (TNBS)-induced colitis with lower expression of some genes encoding inflammation-related cytokines and chemokines in mice. |
| 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. |
