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• 产品描述： TMPA is a high-affinity Nur77 antagonist that binds to Nur77 leading to the release and shuttling of LKB1 in the cytoplasm to activate AMPKα. TMPA effectively lowers blood glucose and attenuates insulin resistance in type II db/db, high-fat diet and streptozotocin-induced diabetic mice. TMPA reduces RICD (restimulation-induced cell death) in human T cells, can also be used in studies of cancer and T-cell apoptosis dysregulation

• 靶点： AMPK;Others; AMPK

• 体外研究：
  TMPA (5, 10, 20, 40, 80 µM; 6 h or 10 µM; 0.5, 1, 3, 6, 12, 24, 36, 48 h) antagonizes the Nur77-LKB1 interaction in a dose- and time-dependent manner in hepatic LO2 cells. TMPA (10 µM; 6 h) enhances the LKB1-AMPKα interaction but decreases the LKB1-Nur77 interaction under physio logical conditions in Lo2 cells. TMPA binds directly to LBD in specific conformation. TMPA (10, 20 µM; 6 h) induces LKB1 nuclear export to activate AMPKα in Lo2 cells. TMPA (10, 50, 100 µM; 4 h) impairs human T-cell RICD (restimulation-induced cell death). Cell Viability Assay Cell Line: T cells Concentration: 10, 50, 100 µM Incubation Time: 4 h Result: Significantly reduced T-cell RICD in a dose-dependent manner. Western Blot Analysis Cell Line: Hepatic LO2 cells Concentration: 10, 20 µM Incubation Time: 6 h Result: Led to an increase of LKB1 phosphorylation at Ser428. Western Blot Analysis Cell Line: Hepatic LO2 cells Concentration: 5, 10, 20, 40, 80 µM Incubation Time: 6 h Result: Increased the amount of phosphorylation of AmPKα in a dose- and time-dependent manner.Rescued the LKB1-AmPKα interaction by reducing the nur77-lKb1 interaction when at 10 µM.

• 体内研究：
  TMPA (50 mg/kg; i.p.; single daily for 19 days) is capable of lowering blood glucose and improving glucose tolerance in type II diabetic mice. Animal Model: Male C57BL/KsJ-Leprdb/Leprdb (db/db) mice (10-week-old; type II diabetic model). Dosage: 50 mg/kg Administration: Intraperitoneal injection; single daily for 19 days. Result: Significantly reduced blood glucose at day 7 and persisted during the remainder of the test.Increased the amount of phosphorylated AMPKα in the liver of mice.

• 参考文献：
  1. Zhan YY, et al. The orphan nuclear receptor Nur77 regulates LKB1 localization and activates AMPK. Nat Chem Biol. 2012 Nov;8(11):897-904. 2. Recher, et al. Modulation of T-cell apoptosis by small molecule compounds targeting the nuclear orphan receptor Nur 77. (2018).

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.628 ml	13.141 ml	26.283 ml
  5 mM	0.526 ml	2.628 ml	5.257 ml
  10 mM	0.263 ml	1.314 ml	2.628 ml
  50 mM	0.053 ml	0.263 ml	0.526 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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