NV-5138
目录号: PL07577 纯度: ≥98.0%
CAS No. :2095886-80-7
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中文名称
NV-5138
英文名称
NV-5138
英文别名
06CA9QMG6Z;4-(difluoromethyl)-L-leucine;N[C@H](C(=O)O)CC(C(F)F)(C)C;((S)-2-Amino-5,5-difluoro-4,4-dimethylpentanoic acid;Pentanoic acid, 2-amino-5,5-difluoro-4,4-dimethyl-, (2S)-;K94;NV-5138
Cas No.
2095886-80-7
分子式
C7H13F2NO2
分子量
181.18
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
NV-5138 是一种亮氨酸类似物,是首个具有选择性的、口服活性的脑内的 mTORC1 的激动剂,与 Sestrin2 结合。NV-5138 可用于抗抑郁的生物研究。
生物活性
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.
性状
Solid
IC50 & Target[1][2]
mTORC1.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: DMSO : 25 mg/mL (137.98 mM; ultrasonic and adjust pH to 2 with HCl)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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