• 产品描述： 4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity)

• 靶点： MT2;MelatoninReceptor; MTReceptor

• 体内研究：
  4-P-PDOT (0.5-1.0 mg/kg; intravenous injection; klotho mutant mice) treatment significantly reverses antioxidant effects mediated by Melatonin. And significantly reverses the changes in the levels of these GSH-related parameters. 4-P-PDOT treatment significantly reverses the memory function of Melatonin-treated klotho mutant mice. 4-P-PDOT also counteracts Melatonin-mediated attenuation in response to the decreases in phospho-ERK expression, Nrf2 nuclear translocation, Nrf2 DNA-binding activity, and GCL mRNA expression in the hippocampi of klotho mutant mice. Animal Model: Klotho mutant mice treatment with Melatonin Dosage: 0.5 mg/kg or 1.0 mg/kg Administration: Intravenous injection Result: Significantly reversed antioxidant effects mediated by Melatonin. Significantly reversed the changes in the levels of these GSH-related parameters. Significantly reversed the memory function of Melatonin-treated klotho mutant mice.

• 参考文献：
  1. Dubocovich ML. Melatonin receptors: are there multiple subtypes? Trends Pharmacol Sci. 1995 Feb;16(2):50-6. 2. hin EJ, et al. Melatonin attenuates memory impairment induced by Klotho gene deficiency via interactive signaling between MT2 receptor, ERK, and Nrf2-related antioxidant potential. Int J Neuropsychopharmacol. 2014 Dec 30;18(6). pii: pyu105. 3. Christopher Browning, et al. Pharmacological characterization of human recombinant melatonin mt1 and MT2 receptors. British Journal of Pharmacology (2000) 129, 877-886. 4. Dubocovich ML, et al. Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor. Naunyn Schmiedebergs Arch Pharmacol. 1997 Mar;355(3):365-75. 5. Roberto Pariente, et al. Participation of MT3 melatonin receptors in the synergistic effect of melatonin on cytotoxic and apoptotic actions evoked by chemotherapeutics. Cancer Chemother Pharmacol. 2017 Nov;80(5):985-998.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	0 ml	0 ml	0 ml
  5 mM	0 ml	0 ml	0 ml
  10 mM	0 ml	0 ml	0 ml
  50 mM	0 ml	0 ml	0 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 *