ITI-214 | PDE | AmBeed-信号通路专用抑制剂

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ITI-214 {[allProObj[0].p_purity_real_show]}

货号：A726292

ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).

ITI-214 化学结构
CAS号：1642303-38-5

ITI-214 3D分子结构
CAS号：1642303-38-5

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ITI-214 纯度/质量文件产品仅供科研

货号：A726292 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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PDE 亚型比较

产品名称	PDE ↓ ↑	PDE1 ↓ ↑	PDE10A ↓ ↑	PDE2 ↓ ↑	PDE3 ↓ ↑	PDE4 ↓ ↑	PDE5 ↓ ↑	PDE6 ↓ ↑	其他靶点	纯度
Doxofylline	✔									99+%
Deltarasin	+++ PDEδ , Kd: 38 nM									99+%
7-(2,3-Dihydroxypropyl)theophylline	✔									98%
Aminophylline	+ PDE, IC50: 0.12 mM									98+%
Anagrelide HCl	✔									99%+
Irsogladine	✔								AChR,mAChR	98%
PF-8380	+++ Autotaxin, IC50: 2.8 nM									99%+
Dipyridamole	✔									98%
Balipodect			++++ PDE10A, IC50: 0.3 nM							99%+
PF-2545920			++++ PDE10A, IC50: 0.37 nM							97%
Luteolin		+ PDE1, Ki: 15.0 μM		++ PDE2, Ki: 6.4 μM	+ PDE3, Ki: 13.9 μM	+ PDE4, Ki: 11.1 μM	+ PDE5, Ki: 9.5 μM			98%
Milrinone				++ PDE2, IC50: 5.2 μM	++ PDE3, IC50: 2.1 μM				ATPase	98%
Pimobendan					++ PDE3, IC50: 0.32 μM					98%
Cilostazol					++ PDE3, IC50: 0.2 μM					98%
Fenspiride HCl					+ PDE3, pIC50: 3.44	+ PDE4, pIC50: 4.16				98%
(S)-(+)-Rolipram						++ PDE4, IC50: 0.75 μM				98%
Apremilast						+++ PDE4, IC50: 74 nM				98%
GSK256066						++++ PDE4B, IC50: 3.2 pM				98+%
Roflumilast						++++ PDE4A4, IC50: 4.3 nM PDE4A1, IC50: 0.7 nM				99%
Rolipram						+++ PDE4B, IC50: 130 nM				99%+
Cilomilast						+++ LPDE4, IC50: 100 nM HPDE4, IC50: 120 nM				98+%
Avanafil							++++ PDE5, IC50: 1 nM			98%
Vardenafil HCl Trihydrate							++++ PDE5, IC50: 0.7 nM			98%
Tadalafil							++++ PDE5, IC50: 1.8 nM			98%
Icariin							++ PDE5, IC50: 0.432 μM			98%
Sildenafil							✔	+++ PDE6, IC50: 33 nM		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

ITI-214 生物活性

描述	ITI-214 is a powerful, CNS-penetrant, orally bioavailable inhibitor of PDE1 (with a Ki of 58 pM), boasting remarkable selectivity over other PDE family enzymes as well as a broad spectrum of enzymes, receptors, transporters, and ion channels. It inhibits recombinant full-length human PDE1A, PDE1B, and PDE1C with Ki values of 33 pM, 380 pM, and 35 pM, respectively. ITI-214 has demonstrated effectiveness in various animal models addressing motor and cognitive functions^[1]^[2].
体内研究	ITI-214 substantially improves memory performance, with a minimum effective dosage identified at 3 mg/kg^[1].
体外研究	ITI-214 exhibits activity that is more than 1000-fold higher against PDE1 isoforms than its closest relative in the PDE family, PDE4D (Ki= 33 nM), and demonstrates 10,000 to 300,000-fold selectivity over all other PDE enzyme families^[2].

ITI-214 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.

ITI-214 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.65mL

0.33mL

0.17mL

8.26mL

1.65mL

0.83mL

16.51mL

3.30mL

1.65mL

ITI-214 技术信息

CAS号	1642303-38-5
分子式	C₂₉H₂₉FN₇O₅P
分子量	605.557

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

DMSO: 30 mg/mL(49.54 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

ITI-214 {[allProObj[0].p_purity_real_show]}

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ITI-214 {[allProObj[0].p_purity_real_show]}

ITI-214 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

ITI-214 质控信息

ITI-214 生物活性

ITI-214 参考文献

ITI-214 实验方案

ITI-214 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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ITI-214 纯度/质量文件产品仅供科研