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 brainmTORC1activator, binding to Sestrin2. NV-5138 is used for antidepressant studies[1][2]. |
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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[1].
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[2].
NV-5138 (80 mg/kg, po, daily for a total of 7 days) also produces antidepressant effects[2].
| Animal Model: | Male Sprague-Dawley rats weighing 250-260 g[2]. | | 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[1]. | | 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. |
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| 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 |
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| 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 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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