| Bioactivity | Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC50 of 0.028 μM. | ||||||||||||
| Target | IC50: 0.028 μM (tryptophan hydroxylase) | ||||||||||||
| Invitro | Telotristat is the active moiety of telotristat etiprate. Telotristat etiprate is an ethyl ester prodrug which is hydrolyzed to telotristat. Telotristat etiprate is orally available serotonin synthesis inhibitor for the treatment of carcinoid syndrome[1]. | ||||||||||||
| In Vivo | Telotristat etiprate is present in very low levels after oral administration. These low levels are due to rapid hydrolysis into the active moiety telotristat. The half-life ranges from approximately 4-12 h. There is no accumulation of telotristat with multiple dose administration over 2 weeks. Exposure to telotristat is approximately dose proportional[1]. | ||||||||||||
| Name | Telotristat | ||||||||||||
| CAS | 1033805-28-5 | ||||||||||||
| Formula | C25H22ClF3N6O3 | ||||||||||||
| Molar Mass | 546.93 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Lapuerta P, et al. Telotristat etiprate, a novel inhibitor of serotonin synthesis for the treatment of carcinoid syndrome. Clin. Invest. (Lond.) (2015) 5(5), 447–456 [2]. US20080153852 |