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• 产品描述： ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions

• 靶点： PDE1:58 pM (Ki);PDE1A:33 pM (Ki);PDE1B:380 pM (Ki);PDE1C:35 pM (Ki);PDE

• 体外研究：
  ITI-214 expresses >1000-fold greater activity toward PDE1 isoforms compared with the next nearest PDE family enzyme, PDE4D (Ki= 33 nM) and 10,000-300,000-fold selectivity toward all other PDE enzyme families

• 体内研究：
  ITI-214 significantly enhances memory performance in the test with a minimum effective dose of 3 mg/kg. Animal Model: Male Sprague-Dawley rats Dosage: 0.1-10 mg/kg Administration: p.o. Result: Significantly enhanced memory performance in the test with a minimum effective dose of 3 mg/kg.

• 参考文献：
  1. Li P, et al. Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases. J Med Chem. 2016;59(3):1149-1164. 2. Snyder GL, et al. Preclinical profile of ITI-214, an inhibitor of phosphodiesterase 1, for enhancement of memory performance in rats. Psychopharmacology (Berl). 2016;233(17):3113-3124.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.651 ml	8.257 ml	16.514 ml
  5 mM	0.33 ml	1.651 ml	3.303 ml
  10 mM	0.165 ml	0.826 ml	1.651 ml
  50 mM	0.033 ml	0.165 ml	0.33 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 *