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ZD 7288

HCN通道抑制剂,ZD7288 是一种有选择性的超极化激活的环核苷酸门控 (HCN) 通道阻断剂

目录号: PC12150 纯度: ≥98%

CAS No. :133059-99-1

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中文名称	ZD 7288
中文别名	N-乙基-1,6-二氢-1,2-二甲基-6-(甲基亚氨基)-N-苯基-4-嘧啶胺盐酸盐;N-乙基-1,6-二氢-1,2-二甲基-6-(甲基亚氨基)-N-苯基-4-嘧啶胺盐酸盐97
英文名称	ZD 7288
英文别名	ZD 7288;N-ethyl-1,2-dimethyl-6-methylimino-N-phenylpyrimidin-4-amine,hydrochloride;N-ethyl-1,6-dihydro-1,2-dimethyl-6-(methylimino)-N-phenyl-4-Pyrimidinamine hydrochloride;Ici-D2788;Oxprenolol hydrochloride;Zeneca ZD7288;ICI D7288;ICI D2788;N-ethyl-1,2-dimethyl-6-methylimino-N-phenyl-pyrimidin-4-amine hydrochl oride;N-Ethyl-1,6-dihydro-1,2-diMethyl-6-(MethyliMino)- N-phenyl-4-pyriMidinaMine Monohydrochloride;ZD7288
Cas No.	133059-99-1
分子式	C₁₅H₂₁N₄Cl
分子量	292.81
包装储存	Sealed and stored at 4℃，, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性	ZD7288 (ICI D7288) is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker.
性状	Solid
IC50 & Target[1][2]	HCN channel
体外研究(In Vitro)	ZD7288 is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker. ZD7288 inhibits glutamate release in a concentration-dependent manner. After incubation with 1, 5 and 50 μM ZD7288 for 24 hours, glutamate content in extracellular fluid is decreased to 69.0±2.8%, 31.4±2.0% and 4.4±0.3%, respectively (P<0.01, vs. DMEM/F12 group [100.2±4.2%]). After incubation with ZD7288 (25, 50, or 100 μM) for 20 minutes, 50 μM glutamate-induced [Ca]_i rises are attenuated to 59.2±2.7%, 41.4±2.3% and 21.0±1.4%, respectively glutamate (P<0.01, vs. 50 μM glutamate group). Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Application of ZD7288 0.1 μM at 5 minutes before high-frequency stimulation significantly decreases the amplitude of field excitatory postsynaptic potentials (fEPSPs), and this inhibitory effect is maintained throughout the recording period. Application of 0.1 μM ZD7288 30 minutes after high-frequency stimulation almost completely reverses the established long-term potentiation (LTP). Following application of ZD7288 (0.1 μM) 5 minutes before high-frequency stimulation, glutamate content is reduced to 74.9±8.0% (P<0.05, vs. normal saline group). Furthermore, application of 0.1 μM ZD7288 30 minutes after high-frequency stimulation markedly decreases the glutamate content to 77.0%±9.4% (P<0.05, vs. normal saline group). Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature or refrigerated transportation.
储存方式	Sealed and stored at 4℃，, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Zhang XX, et al. ZD7288, a selective hyperpolarization-activated cyclic nucleotide-gated channel blocker, inhibits hippocampal synaptic plasticity. Neural Regen Res. 2016 May;11(5):779-86. [Information]

溶解度数据

体外研究:

DMSO : 50 mg/mL (170.76 mM; Need ultrasonic)

H₂O : ≥ 50 mg/mL (170.76 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.4152 mL	17.0759 mL	34.1518 mL
5 mM	0.6830 mL	3.4152 mL	6.8304 mL
10 mM	0.3415 mL	1.7076 mL	3.4152 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： PBS
Solubility: 100 mg/mL (341.52 mM); Clear solution; Need ultrasonic

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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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