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
ZD 7288是一种超极化激活环核苷酸门控（HCN）通道阻滞剂。
Cas No.:133059-99-1
Sample solution is provided at 25 µL, 10mM.
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ZD 7288 is a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker [1]. ZD 7288 reduces cellular spontaneous activity and excitability by reducing If/Ih currents [2]. ZD 7288 is commonly used in areas such as arrhythmias, neuropathic pain, or irritable bowel syndrome (IBS) [3-4].
In mouse embryonic stem cells, ZD 7288 (0.1-30μM; 72h) decreased the proportion of cells in G0/G1 phase and increase the proportion of cells in S phase [5]. In HEK293 cells, ZD 7288 (0.1-100μM; 2h) inhibits Na+ currents in cells transfected with Nav 1.4 plasmid [6]. In α-TC6 cells, blocking HCN channels with ZD 7288 (100μM; 30min) significantly increases the intracellular calcium concentration [7].
In shrews, ZD 7288 (0-1mg/kg; ip; single injection) induces vomiting in a dose-dependent manner [8]. In C57BL/6 mice, ZD 7288 (6.25μg/kg, 12.5μg/kg; ip; single injection) inhibits sevoflurane-induced agitation [9].
References:
[1]. Zhang X, Min X, Xu X, et al. ZD7288, a selective hyperpolarization-activated cyclic nucleotide-gated channel blocker, inhibits hippocampal synaptic plasticity[J]. Neural Regeneration Research, 2016, 11(5): 779-786.
[2]. Gasparini S, DiFrancesco D. Action of the hyperpolarization-activated current (I h) blocker ZD 7288 in hippocampal CA1 neurons[J]. Pflügers Archiv, 1997, 435(1): 99-106.
[3]. Chen Y, Lin C, Tang Y, et al. ZD 7288, an HCN channel blocker, attenuates chronic visceral pain in irritable bowel syndrome-like rats[J]. World journal of gastroenterology: WJG, 2014, 20(8): 2091.
[4]. Yang L, Liu X, Yao K, et al. HCN channel antagonist ZD7288 ameliorates neuropathic pain and associated depression[J]. Brain Research, 2019, 1717: 204-213.
[5]. Lau Y T, Wong C K, Luo J, et al. Effects of hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blockers on the proliferation and cell cycle progression of embryonic stem cells[J]. Pflügers Archiv-European Journal of Physiology, 2011, 461(1): 191-202.
[6]. Wu X, Liao L, Liu X, et al. Is ZD7288 a selective blocker of hyperpolarization-activated cyclic nucleotide-gated channel currents?[J]. Channels, 2012, 6(6): 438-442.
[7]. Zhang Y, Zhang N, Gyulkhandanyan A V, et al. Presence of functional hyperpolarisation-activated cyclic nucleotide-gated channels in clonal alpha cell lines and rat islet alpha cells[J]. Diabetologia, 2008, 51(12): 2290-2298.
[8]. Zhong W, Darmani N A. The Hcn Channel blocker Zd7288 induces Emesis in the least shrew (Cryptotis parva)[J]. Frontiers in Pharmacology, 2021, 12: 647021.
[9]. Liang P, Xu-Bin H, Feng-Shan L, et al. Hyperpolarization-Activated Cyclic Nucleotide-Gated Channel Blocker ZD7288 Prevents Sevoflurane-Induced Hyperactivity in A Novel Mice Behavioral Model[J]. Journal of Anesthesia and Perioperative Medicine (JAPM), 2017, 4(5): 205.
ZD 7288是一种超极化激活环核苷酸门控（HCN）通道阻滞剂 [1]。ZD 7288通过降低If/Ih电流来降低细胞自发活动和兴奋性 [2]。ZD 7288常用于治疗心律失常、神经性疼痛或肠易激综合征（IBS） [3-4]。
在小鼠胚胎干细胞中，ZD 7288（0.1-30μM；72h）降低G0/G1期细胞的比例，并增加了S期细胞的比例 [5]。在HEK293细胞中，ZD 7288（0.1-100μM；2h）抑制了转染Nav 1.4质粒的细胞中的Na+电流 [6]。在α-TC6细胞中，用ZD 7288（100μM；30min）阻断HCN通道可显著升高细胞内钙离子浓度 [7]。
在鼩鼱中，ZD 7288（0-1mg/kg；ip；单次注射）以剂量依赖性方式诱发呕吐 [8]。在C57BL/6小鼠中，ZD 7288（6.25μg/kg，12.5μg/kg；ip；单次注射）可抑制七氟醚引起的躁动 [9]。
| Cell experiment [1]: | |
Cell lines | Mouse embryonic stem cells (mESCs) |
Preparation Method | Cell proliferation was determined in 24-well plates by simple cell counting techniques. mESCs were treated with different concentrations of ZD 7288 for the entire period of the experiments. Medium was changed daily. Cells were collected at different time points for cell counting. Cells treated with equal volume of water (solvent for ZD 7288) were used as control. Numbers of viable and nonviable cells were determined by trypan blue exclusion assay. |
Reaction Conditions | 0.1-30μM; 72h |
Applications | ZD 7288 decreased the proportion of cells in G0/G1 phase and increase the proportion of cells in S phase. |
| Animal experiment [2]: | |
Animal models | Shrews |
Preparation Method | Daily food restriction was initiated 2 hours before the start of the experiment, but before the injection of the emetic, each shrew was given 3-4 mealworms to aid in the identification of wet vomit, as previously reported. For systemic dose-response emesis studies, groups of shrews were injected with different doses of ZD 7288 (0, 0.05, 0.25, and 1mg/kg, intraperitoneally, n = 8 shrews per group). |
Dosage form | 0-1mg/kg; ip; single injection |
Applications | ZD 7288 induces vomiting in a dose-dependent manner. |
References: | |
| 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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