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产品描述： Taltirelin is at thyrotropin-releasing hormone receptor (TRH-R) superagonist (IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca2+ concentration (Ca2+ release)) |
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靶点：
Thyroid hormone receptor(THR);Thyroidhormonereceptor(THR) |
体内研究：
Taltirelin (TAL), in mouse models of CRF.To model fatigue, we used a mouse model of chemotherapy, a mouse model of radiation therapy, and mice bearing colon 26 carcinoma tumors.?We used the treadmill fatigue test to assess fatigue-like behavior after treatment with TAL.Additionally, we used wild-type and TRH receptor knockout mice to determine which TRH receptor was necessary for the actions of TAL.Tumor-bearing mice displayed muscle wasting and all models caused fatigue-like behavior, with mice running a shorter distance in the treadmill fatigue test than controls.?TAL reversed fatigue-like behavior in all three models and the mouse TRH1 receptor was necessary for the effects of TAL.These data suggest that TAL may be useful in alleviating fatigue in all cancer patients and provide further support for evaluating TAL as a potential therapy for CRF in humans |
参考文献：
1. Thirunarayanan N, et al. Taltirelin is a superagonist at the human thyrotropin-releasing hormone receptor. Front Endocrinol (Lausanne). 2012 Oct 9;3:120. 2. Dougherty J P , Wolff B S , Cullen M J , et al. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue.[J]. Pharmacological Research, 2017, 124:1-8. |
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溶解性：
Soluble in DMSO |
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保存条件：
-20℃ |
配置溶液浓度参考：
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1mg |
5mg |
10mg |
| 1 mM |
2.467 ml |
12.333 ml |
24.667 ml |
| 5 mM |
0.493 ml |
2.467 ml |
4.933 ml |
| 10 mM |
0.247 ml |
1.233 ml |
2.467 ml |
| 50 mM |
0.049 ml |
0.247 ml |
0.493 ml |
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| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京