| 產(chǎn)品描述： | Telotristat etiprate (LX1606 Hippurate) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production. |
| 靶點(diǎn)： |
Tryptophan Hydroxylase;Hydroxylase |
| 體內(nèi)研究： |
Telotristat ethyl (15, 50, 150, 300 mg/kg, po, qd) reduces serotonin content in the periphery, but not in the brain of the mice. Telotristat ethyl (200 mg/kg po, qd) prevents the increase in blood neutrophil counts that is observed after TNBS challenge, provides significant protection in a mouse model of inflammatory bowel disease. Telotristat ethyl (200 mg/kg po, qd) protects the mouse IBD model confirmed by histopathology evaluation. Telotristat ethyl (15, 50, 150, 300 mg/kg) depletes 5-HT from the jejunum but not the brain. But Telotristat ethyl (200 mg/kg, p.o.) does not deplete enteric neuronal serotonin (5-HT), or alter constitutive gastrointestinal motility in mice. Telotristat ethyl (200 mg/kg) alleviates the severity of trinitrobenzene sulfonic acid (TNBS)-induced colitis |
| 參考文獻(xiàn)： |
1. Tamas Oravecz, et al. LX1606 (aka LX1032), a Novel Inhibitor of Serotonin Synthesis, Alleviates Development of Inflammatory Bowel Disease in a Preclinical Model. 2. Margolis, K.G., et al., Pharmacological reduction of mucosal but not neuronal serotonin opposes inflammation in mouse intestine. Gut, 2013. |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
避光;-20°C |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.326 ml |
6.63 ml |
13.26 ml |
| 5 mM |
0.265 ml |
1.326 ml |
2.652 ml |
| 10 mM |
0.133 ml |
0.663 ml |
1.326 ml |
| 50 mM |
0.027 ml |
0.133 ml |
0.265 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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