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產品描述： NV-5138, a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. NV-5138 is used for antidepressant studies |
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靶點：
mTORC1;mTOR |
體內研究：
NV-5138 is found to be essentially 100% orally bioavailable with an elimination half-life in plasma of ~ 3 h determined following intravenous and oral dosing in rats. NV-5138 (160 mg/kg, po, single dose) rapidly increases levels of phospho-mTOR as well as the downstream targets, phospho-p70S6K1, and phosphor-4EB-P1, in synaptosomal preparations of PFC. NV-5138 (80 mg/kg, po, daily for a total of 7 days) also produces antidepressant effects. Animal Model: Male Sprague-Dawley rats weighing 250-260 g. Dosage: 40, 80, 160 mg/kg. Administration: PO, single dose (160 mg/kg) or daily for a total of 7 days (40, 80 mg/kg). Result: Produced antidepressant effects. Animal Model: Male Sprague–Dawley (SD) rats weighed 250-400 g. Dosage: 1 mg/kg, 5 mg/kg (Pharmacokinetic Design). Administration: I.V at 1 mg/kg and PO at 5 mg/kg. Result: Essentially 100% orally bioavailable with an elimination half-life in plasma of ~ 3 h. |
參考文獻：
1. Sengupta S, et al. Discovery of NV-5138, the first selective Brain mTORC1 activator. Sci Rep. 2019 Mar 11;9(1):4107. 2. Kato T, et al. Sestrin modulator NV-5138 produces rapid antidepressant effects via direct mTORC1 activation. J Clin Invest. 2019 Apr 16;129(6):2542-2554. |
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溶解性：
Soluble in DMSO |
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保存條件：
-20℃ |
配置溶液濃度參考：
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1mg |
5mg |
10mg |
| 1 mM |
5.519 ml |
27.596 ml |
55.193 ml |
| 5 mM |
1.104 ml |
5.519 ml |
11.039 ml |
| 10 mM |
0.552 ml |
2.76 ml |
5.519 ml |
| 50 mM |
0.11 ml |
0.552 ml |
1.104 ml |
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| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業執照(三證合一)
北京