Telotristat

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Chemical Structure| 1033805-28-5 同义名 : LP-778902
CAS号 : 1033805-28-5
货号 : A660906
分子式 : C25H22ClF3N6O3
纯度 : 99%
分子量 : 546.929
MDL号 : MFCD20528907
存储条件：

Pure form Keep in dark place,Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(63.99 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The dysfunction of the peripheral serotonin (5-hydroxytryptamine, 5-HT) system is involved in many diseases, such as carcinoid syndrome, fibrotic disease, atherosclerosis, and pulmonary arterial hypertension. Tryptophan hydroxylase 1 (TPH1) is an aromatic amino acid hydroxylase essential for the biosynthesis of peripheral 5-HT. Telotristat etiprate is the ester prodrug of a potent TPH1 inhibitor, LX-1033, with an IC50 value of 16nM[2]. Telotristat (also known as LP778902) is the active moiety of telotristat etiprate. In C57BL/6 mice, telotristat (~100 mg/kg) supplementation significantly reduced maternal serum serotonin concentration compared with the control dams on day 1 and day 21 of lactation, but did not change serum serotonin level in their pups. Maternal supplementation with telotristat did not significantly alter the ratio of maternal femoral trabecular bone volume to tissue volume. Pups of the dams treated with telotristat showed a reduced ratio of bone volume to tissue volume on the day of weaning, fewer and thinner trabeculae, and increased trabecular spacing compared with control pups. Pups born to telotristat-supplemented dams also had reduced total serum calcium on day 21 of lactation[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.14mL

1.83mL

0.91mL

18.28mL

3.66mL

1.83mL
参考文献

[1]Margolis KG, Stevanovic K, et al. Pharmacological reduction of mucosal but not neuronal serotonin opposes inflammation in mouse intestine. Gut. 2014 Jun;63(6):928-37.

[2]Goldberg DR, De Lombaert S, Aiello R, Bourassa P, Barucci N, Zhang Q, Paralkar V, Stein AJ, Valentine J, Zavadoski W. Discovery of acyl guanidine tryptophan hydroxylase-1 inhibitors. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2855-2860.

[3]Weaver SR, Fricke HP, Xie C, Aiello RJ, Charles JF, Hernandez LL. Peripartum dietary supplementation of a small-molecule inhibitor of tryptophan hydroxylase 1 compromises infant, but not maternal, bone. Am J Physiol Endocrinol Metab. 2018;315(6):E1133-E1142.