ZD 7288 (Synonyms: ICI-D 7288) |
Catalog No.GC10578
One-Click Copy Product Info
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ZD 7288 is a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| Synonyms | ICI-D 7288 | ||
| Chemical Name | (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 | ||
| Formula | C15H21ClN4 | M.Wt | 292.81 |
| Solubility | 50mg/mL in ethanol, 30mg/mL in DMSO or DMF;Water : ≥ 50 mg/mL (170.76 mM) | Storage | Store at 2-8°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4152 mL | 17.0759 mL | 34.1518 mL |
| 5 mM | 683 μL | 3.4152 mL | 6.8304 mL |
| 10 mM | 341.5 μL | 1.7076 mL | 3.4152 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)