ZD 7288
(Synonyms: 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,ICI-D 7288) 目录号 : GC10578
An HCN channel blocker
Cas No.:133059-99-1
Sample solution is provided at 25 µL, 10mM.
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ZD 7288 is an inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channel [1].
The HCN channel is found in the sinoatrial node (SAN) and is permeable to both Na+ and K+. The HCN current exists in neurons under hyperpolarization of the cell membrane and plays an important role in neuropathic pain [1].
In CA1 pyramidal cells from Wistar rats, ZD 7288 inhibited T-type Ca2+ channel currents in a concentration-dependant way [2]. In neonatal rat facial motoneurones, ZD-7288 (0.1-10 μM) inhibited the hyperpolarisation-activated current with IC50 value of 0.2 μM in a time- and voltage-dependent way [3]. In CA1 pyramidal neurons, ZD 7288 (1-1000 μM) inhibited the hyperpolarization-activated current. However, ZD 7288 had no influence on long-term depression (LTD) of the CA3-CA1 synapse [4].
In rats with chronic visceral pain, ZD 7288 (50-100 nM) significantly inhibited abdominal withdrawal reflex (AWR) scores and electromyographic (EMG) responses. Also, ZD 7288 significantly increased pain thresholds. These results suggested that spinal HCN channels might play a critical role in chronic visceral pain [1].
References:
[1]. Chen Y, Lin C, Tang Y, et al. ZD 7288, an HCN channel blocker, attenuates chronic visceral pain in irritable bowel syndrome-like rats. World J Gastroenterol, 2014, 20(8): 2091-2097.
[2]. Sánchez-Alonso JL, Halliwell JV, Colino A. ZD 7288 inhibits T-type calcium current in rat hippocampal pyramidal cells. Neurosci Lett, 2008, 439(3): 275-280.
[3]. Larkman PM, Kelly JS. Modulation of the hyperpolarisation-activated current, Ih, in rat facial motoneurones in vitro by ZD-7288. Neuropharmacology, 2001, 40(8): 1058-1072.
[4]. Gasparini S, DiFrancesco D. Action of the hyperpolarization-activated current (Ih) blocker ZD 7288 in hippocampal CA1 neurons. Pflugers Arch, 1997, 435(1): 99-106.
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Cell experiment: |
Primary hippocampal neurons are obtained from neonatal (1 to 2 day-old) Sprague-Dawley rats, and used in this study. The cells are incubated for 24 hours with ZD7288 (1, 5, or 50 µM), 8-bromoadenosine cyclic adenosine monophosphate (8-Br-cAMP, 5 or 50 µM), or forskolin (1 or 5 µM), and the culture medium is collected for glutamate measurement[1]. |
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Animal experiment: |
Specific-pathogen-free adult male Sprague-Dawley rats, aged 10 weeks and weighing 200±20 g are used in this study. For hippocampal administration of saline or drugs, a cannula is carefully inserted into the CA3 area with an introductory tube fixed parallel to the recording electrode, reaching 0.1 to 0.2 mm higher than the electrode tip. To test the effects of blockers on the induction of long-term potentiation (LTP), 0.1 µM ZD7288 or the monovalent cation cesium (Cs+) is applied 5 minutes before high-frequency stimulation. To test the effects of blockers on the maintenance of LTP, ZD7288/Cs+ is slowly administered using an infusion/withdrawal pump 30 minutes after the high-frequency stimulation[1]. |
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References: [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. |
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| Cas No. | 133059-99-1 | SDF | |
| 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,ICI-D 7288 | ||
| 化学名 | (E)-N-ethyl-1,2-dimethyl-6-(methylimino)-N-phenyl-1,6-dihydropyrimidin-4-amine hydrochloride | ||
| Canonical SMILES | CCN(C1=CC=CC=C1)C2=C/C(N(C)C(C)=N2)=N\C.Cl | ||
| 分子式 | C15H21ClN4 | 分子量 | 292.81 |
| 溶解度 | 50mg/mL in ethanol, 30mg/mL in DMSO or DMF;Water : ≥ 50 mg/mL (170.76 mM) | 储存条件 | Store at 2-8°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4152 mL | 17.0759 mL | 34.1518 mL |
| 5 mM | 0.683 mL | 3.4152 mL | 6.8304 mL |
| 10 mM | 0.3415 mL | 1.7076 mL | 3.4152 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet