NV-5138,98.0%

产品编号:Bellancom-114384| CAS NO:2095886-80-7| 分子式:C7H13F2NO2| 分子量:181.18

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-114384
2500.00 杭州 北京(现货)
Bellancom-114384
4000.00 杭州 北京(现货)
Bellancom-114384
8500.00 杭州 北京(现货)
Bellancom-114384
13500.00 杭州 北京(现货)
Bellancom-114384
19500.00 杭州 北京(现货)

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NV-5138

产品介绍 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.

体外研究
体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
性状Solid
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (137.98 mM; ultrasonic and adjust pH to 2 with HCl)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 5.5194 mL 27.5969 mL 55.1937 mL
5 mM 1.1039 mL 5.5194 mL 11.0387 mL
10 mM 0.5519 mL 2.7597 mL 5.5194 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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
-20°C 1 month
参考文献

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