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Telotristat

CAS No. : 1033805-28-5

MCE 站：Telotristat

产品活性：Telotristat (LP-778902) 是一种有效的色氨酸羟化酶 (tryptophan hydroxylase) 抑制剂，在体内的 IC₅₀ 值为0.028 μM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Tryptophan Hydroxylase

In Vitro: 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.

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.

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