Telotristat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Telotristat (LP-778902) 是一种有效的外周血清素合成小分子抑制剂，通过抑制色氨酸羟化酶 (TPH) 发挥作用，IC50 为 28 nM。

Telotristat (LP-778902) is a potent, small-molecule inhibitor of peripheral serotonin synthesis, acts by inhibiting tryptophan hydroxylase (TPH) with IC50 of 28 nM, demonstrates potential for the treatment of carcinoid syndrome.Gastric Cancer Approved.

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.

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.

LP778902 | LP 778902 | LP-778902

Metabolic Enzyme/Protease

TPH

TPH

Cancer

Gastric Cancer

1033805-28-5

546.9288

C25H22ClF3N6O3

>98% (HPLC)

10 mM in DMSO

CC1=NN(C=C1)C2=C(C=CC(=C2)Cl)C(C(F)(F)F)OC3=NC(=NC(=C3)C4=CC=C(C=C4)CC(C(=O)O)N)N

L-Phenylalanine, 4-[2-amino-6-[(1R)-1-[4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]-4-pyrimidinyl]-

(-20℃)

With Ice Pack

≥ 2 years