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• 产品描述： Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia

• 靶点： 5-HT2A Receptor:0.54 nM (Ki);DopamineReceptor; 5-HTReceptor

• 体外研究：
  Lumateperone (2-30 μM) tosylate has anti-tumor activity and can inhibit cell proliferation in a dose-dependent manner. Cell Proliferation Assay Cell Line: RPMI-8226 cells Concentration: 2-30 μM Incubation Time: Result: Inhibited cell growth with the IC50 value of 17.30 μM.

• 体内研究：
  Lumateperone (i.p., 1-10 mg/kg) tosylate promotes NMDA and AMPA-induced currents in a dopamine D 1 receptor-dependent manner and increases the release of dopamine and glutamate in rat mPFC slices. Animal Model: Adult male Sprague-Dawley rats Dosage: 1-10 mg/kg Administration: Intraperitoneal injection Result: Inhibited avoidance response at concentrations of 1, 3 and 10 mg/kg after 20 minutes.Promoted NMDA and AMPA-sensitive currents, also significantly increased dopamine and glutamate release at 10 mg/kg in mPFC cone cells of rat.

• 参考文献：
  1. Jinyuan Zhang, et al. Identification of Trovafloxacin, Ozanimod, and Ozenoxacin as Potent c-Myc G-quadruplex Stabilizers to Suppress c-Myc Transcription and Myeloma Growth. Mol Inform. 2022 Mar 30:e2200011. 2. J Titulaer, et al. Lumateperone-mediated effects on prefrontal glutamatergic receptor-mediated neurotransmission: A dopamine D1 receptor dependent mechanism. Eur Neuropsychopharmacol. 2022 Jul 22;62:22-35. 3. Lumateperone

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.768 ml	8.839 ml	17.677 ml
  5 mM	0.354 ml	1.768 ml	3.535 ml
  10 mM	0.177 ml	0.884 ml	1.768 ml
  50 mM	0.035 ml	0.177 ml	0.354 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 *