| 产品描述: | LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally. |
| 靶点: |
Tryptophan Hydroxylase;Hydroxylase; LPAReceptor |
| 体内研究: |
With oral administration of LX-1031 in mice, the average 5-HT reductions in the jejunum relative to control are appr 33, 51, and 66% with the 15, 45 and 135 mg/kg/day doses respectively. In a preliminary report, the effects of LX-1031, 100 mg/kg daily, on 5-HT levels in jejunal mucosa are reversible within 2 days of discontinuation in mice. LX-1031 dose-dependently reduces expression of 5-HT in the duodenum, jejunum and ileum, but has no effect on brain 5-HT levels in preclinical assay |
| 参考文献: |
1. Camilleri M. LX-1031, a tryptophan 5-hydroxylase inhibitor, and its potential in chronic diarrhea associated with increased serotonin. Neurogastroenterol Motil. 2011 Mar;23(3):193-200. 2. Camilleri M. LX-1031, a tryptophan 5-hydroxylase inhibitor that reduces 5-HT levels for the potential treatment of irritable bowel syndrome. IDrugs. 2010 Dec;13(12):921-8. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.857 ml |
9.285 ml |
18.569 ml |
| 5 mM |
0.371 ml |
1.857 ml |
3.714 ml |
| 10 mM |
0.186 ml |
0.928 ml |
1.857 ml |
| 50 mM |
0.037 ml |
0.186 ml |
0.371 ml |
|
| 注意: |
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