• 產(chǎn)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

• 靶點(diǎn)： mTORC1;mTOR

• 體內(nèi)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(xiàn)：
  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.

• 溶解性： Soluble  in  DMSO

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	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

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *