Telotristat

目录号: GC16279纯度: >98%同义词: LP778902

A TPH1 inhibitor

Cas No.: 1033805-28-5

规格	价格	库存	数量
1mg	¥475.00	现货	1
5mg	¥1,324.00	现货	1
10mg	¥1,987.00	现货	1
25mg	¥3,604.00	现货	1
50mg	¥5,821.00	现货	1
10mM (in 1mL DMSO)	¥1,418.00	现货	1

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文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例

Nature
641, 529–536 (2025)
Nature
628, 630–638 (2024)
Nature
632, 686–694 (2024)
Nature
618, 1017–1023 (2023)
Nature
610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
Science
388(6745) (2025)
Science
387(6739) (2025)
Science
387(6734) (2025)
Cell Research
35, 97–116 (2025)
Cell Research
34, 683–706 (2024)
Cell Research
33, 273–287 (2023)
Cell Research
33, 546–561 (2023)
Cell Research
33, 904–922 (2023)
Cell Research
31, 1291–1307 (2021)

产品描述 Description

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).

实验参考方法 Experimental Reference Method

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°C 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].

References:

[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

产品文档 Product Documents

Purity:>98%

COA SDS Data Sheet

化学性质Chemical Properties

CAS 号

1033805-28-5

同义词

LP778902

化学名

(2S)-2-amino-3-[4-[2-amino-6-[(1R)-1-[4-chloro-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]pyrimidin-4-yl]phenyl]propanoic acid

SMILES

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

分子式

C₂₅H₂₂ClF₃N₆O₃

分子量

546.93 g/mol

溶解性

0.5mg/mL in ethanol, 10mg/mL in DMSO, or DMF

保存条件

Store at -20°C

General tips

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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