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Telotristat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Telotristat图片
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
Telotristat (LP-778902) 是一种有效的色氨酸羟化酶抑制剂,体内 IC50 为 0.028 μM。

Cell experiment:

BON CBA cells are grown in equal volume of DMEM and F12K with 5% bovine serum for 3-4 hours (20 K cell/well) and telotristat is added at a concentration range of 0.07 to 50 μM. The cells are incubated at 37℃ overnight. 50 μM of the culture supernatant is then taken for 5HTP measurement. The supernatant is mixed with equal volume of 1M TCA, then filtered through glass fiber. The filtrate is loaded on reverse phase HPLC for 5HTP concentration measurement. The cell viability is measured by treating the remaining cells with Celltiter-Glo Luminescent Cell Viability Assay[2].

Animal experiment:

Rats: 14-week-old male C57 albino mice are dosed once daily by oral gavage at 5-10 mL/kg for four consecutive days. Five hours after the last dose, the animals are quickly sacrificed. 5-HT is extracted from the blood or tissues and measured by HPLC. Blood samples are taken for exposure analysis[2].

产品描述

Telotristat is a tryptophan hydroxylase 1 (TPH1) inhibitor (IC50 = 16 nM).[1] Dietary administration of telotristat to pregnant and lactating mice decreases serotonin levels in maternal serum and decreases the femoral bone volume to tissue volume ratio, trabecular number and thickness, and cortical tissue mineral density, as well as serum calcium levels, in pups.[2]

Reference:
[1]. Goldberg, D.R., De Lombaert, S., Aiello, R., et al. Discovery of acyl guanidine tryptophan hydroxylase-1 inhibitors. Bioorg. Med. Chem. Lett. 26(12), 2855-2860 (2016).
[2]. Weaver, S.R., Fricke, H.P., Xie, C., et al. Peripartum dietary supplementation of a small-molecule inhibitor of tryptophan hydroxylase 1 compromises infant, but not maternal, bone. Am. J. Physiol. Endocrinol. Metab. 215(6), E1133-E1142 (2018).