ITI-214|1642303-38-5|-陌孚医药/Medlife

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ITI-214

目录号: PL09703 纯度: ≥99%

CAS No. :1642303-38-5

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中文名称	ITI-214
英文名称	ITI-214
英文别名	ITI214;ITI-214;YP683YZB8K;(6aR,9aS)-2-(4-(6-fluoropyridin-2-yl)benzyl)-5-methyl-3-(phenylamino)-5,6a,7,8,9,9a-hexahydrocyclopenta[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one phosphate;Lenrispodun phosphate;PDE1-IN-1 (phosphate);Lenrispodun phosphate [USAN];Cyclopent(4,5)imidazo(1,2-a)pyrazolo(4,3-E)pyrimidin-4(2H)-one, 2-((4-(6-fluoro-2-pyridin;ITI-214 phosphate
Cas No.	1642303-38-5
分子式	C₂₉H₂₉FN₇O₅P
分子量	605.56
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

ITI-214 是一种有效的中枢神经系统活性抑制剂，具有口服生物活性的 PDE1 抑制剂 (K_i of 58 pM)，对其他 PDE 家族成员和一系列酶、受体、转运体和离子通道具有良好的选择性。ITI-214 分别以 33 pM、380 pM 和 35 pM 的K_i 抑制重组人 PDE1A、PDE1B 和 PDE1C。ITI-214 在各种运动和认知功能的动物模型中显示出有效性。

生物活性

ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (K i 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 K i s of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions.

性状

Solid

IC50 & Target[1][2]

PDE1 58 pM (Ki) PDE1A 33 pM (Ki)

体外研究(In Vitro)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

ITI-214 significantly enhances memory performance in the test with a minimum effective dose of 3 mg/kg. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : ≥ 30 mg/mL (49.54 mM)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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