| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S82151-5mg促销 |
≥98% | ￥3500.00 ￥1900.00 |
货期：3-5天 | - | - | - | - |
|
S82151-10mg促销 |
≥98% | ￥5000.00 ￥3500.00 |
货期：3-5天 | - | - | - | - |
|
| 产品描述： | ITI-214 free base 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 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions | ||||||||||||||||||||
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| 靶点： | PDE1:58 pM (Ki);PDE1A:33 pM (Ki);PDE1B:380 pM (Ki);PDE1C:35 pM (Ki);Others | ||||||||||||||||||||
| 体外研究： | ITI-214 is found to potently inhibit the activity of full-length recombinant r-hPDE1A (Ki= 34 pM), r-hPDE1B (Ki= 380 pM), and r-hPDE1C (Ki= 37 pM) enzymes transiently expressed in HEK cells. The compound expressed >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. 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 Feb 11;59(3):1149-64. 2. Lawrence Wennogle. Novel uses. From PCT Int. Appl. (2014), WO 2014145617 A2 20140918. 3. Peng Li , et al. Salt crystals. From PCT Int. Appl. (2013), WO 2013192556 A2 20131227. 4. Allen A. Fienberg, et al. Organic compounds. From PCT Int. Appl. (2010), WO 2010132127 A1 20101118. | ||||||||||||||||||||
| 溶解性： | 10 mM in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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