ZD7288
Based on 9 publication(s) in Google Scholar
ZD7288 (ICI D7288) is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker.
For research use only. We do not sell to patients.
- Purity: 99.77%
- CAS No.: 133059-99-1
- Formula: C15H21ClN4
- Molecular Weight:292.81
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ZD7288
More- J Headache Pain. 2023 Apr 21;24(1):44. [Abstract]
- J Affect Disord. 2023 Mar 1:324:143-152. [Abstract]
- Int J Mol Sci. 2024 Nov 7;25(22):11971. [Abstract]
- Neuropharmacology. 2025 Jun 1:270:110371. [Abstract]
- Neuropharmacology. 2020 Oct 1:176:108222. [Abstract]
- iScience. 2024 Sep 13;27(10):110955. [Abstract]
- bioRxiv. 2023 Mar 5.
- Research Square Print. October 6th, 2022.
- Oxid Med Cell Longev. 2022 Feb 10;2022:4299892. [Abstract]
Customer Validation & Images
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In Vivo Efficacy Study
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WB
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IF
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In Vivo Efficacy Study
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Biological Activity
HCN channel[1]
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 [Ca2+]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)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 133059-99-1
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Appearance Solid
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Molecular Weight 292.81
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Formula C15H21ClN4
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Color White to off-white
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SMILES
[H]Cl.C/N=C1C=C(N(CC)C2=CC=CC=C2)N=C(C)N/1C
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Synonyms
ICI D7288
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (9)
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Journal Impact Factor
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Most Recent
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J Headache Pain
Activation of CB1R alleviates central sensitization by regulating HCN2-pNR2B signaling in a chronic migraine rat model. [Abstract]2023 Apr 21;24(1):44. PMID: 37085778
ZD7288 purchased from MedChemExpress. Usage Cited in: J Headache Pain. 2023 Apr 21;24(1):44. [Abstract]
ZD 7288 (5 μg; i.c.) markedly improved mechanical pain thresholds of the periorbital region and hindpaw of CM rats.
ZD7288 purchased from MedChemExpress. Usage Cited in: J Headache Pain. 2023 Apr 21;24(1):44. [Abstract]
ZD 7288 (5 μg; i.c.) substantially repressed the expression of pNR2B, CaMKII, and pCREB in CM rats.
ZD7288 purchased from MedChemExpress. Usage Cited in: J Headache Pain. 2023 Apr 21;24(1):44. [Abstract]
ZD 7288 (5 μg; i.c.) robustly reduced the number of c-Fos-positive cells and the average fluorescence intensity of CGRP and SP in CM mice.
ZD7288 purchased from MedChemExpress. Usage Cited in: J Headache Pain. 2023 Apr 21;24(1):44. [Abstract]
ZD 7288 (5 μg; i.c.) abolished the AM 251-evoked decline in the mechanical pain thresholds of the periorbital region in CM rats.
ZD7288 purchased from MedChemExpress. Usage Cited in: J Headache Pain. 2023 Apr 21;24(1):44. [Abstract]
ZD 7288 (5 μg; i.c.) reversed the AM 251-induced elevation of pNR2B, CGRP, and c-Fos expression in CM rats.
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J Affect Disord
Prenatal alcohol exposure enhanced alcohol preference and susceptibility to PTSD in a sex-dependent manner through the synaptic HCN1 channel. [Abstract]2023 Mar 1:324:143-152. PMID: 36587902
ZD7288 purchased from MedChemExpress. Usage Cited in: J Affect Disord. 2023 Mar 1:324:143-152. [Abstract]
In the prefrontal cortex (PFC) region, ZD7288 (1, 2 μg/mL; i.c.v) significantly ameliorates PAE-induced increases in synaptic HCN1 expression in mice.
ZD7288 purchased from MedChemExpress. Usage Cited in: J Affect Disord. 2023 Mar 1:324:143-152. [Abstract]
ZD7288 (1, 2 μg/mL; i.c.v) decreases BDNF expression and TrkB phosphorylation in the hippocampus regions of mice.
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Int J Mol Sci
Glucocorticoids Selectively Inhibit Hippocampal CA1 Pyramidal Neurons Activity Through HCN Channels. [Abstract]2024 Nov 7;25(22):11971. PMID: 39596039 -
Neuropharmacology
Inhibition of HCN channels decreases motivation for alcohol and deprivation-induced drinking in alcohol preferring rats. [Abstract]2025 Jun 1:270:110371. PMID: 39983913 -
Neuropharmacology
Chronic morphine induces cyclic adenosine monophosphate formation and hyperpolarization-activated cyclic nucleotide-gated channel expression in the spinal cord of mice. [Abstract]2020 Oct 1:176:108222. PMID: 32659289 -
iScience
T cell death-associated gene 8-mediated distinct signaling pathways modulate the early and late phases of neuropathic pain. [Abstract]2024 Sep 13;27(10):110955. PMID: 39381739 -
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Oxid Med Cell Longev
Effect of Shenfu Injection on Differentiation of Bone Marrow Mesenchymal Stem Cells into Pacemaker-Like Cells and Improvement of Pacing Function of Sinoatrial Node. [Abstract]2022 Feb 10;2022:4299892. PMID: 35186186
Solvent & Solubility
DMSO : 50 mg/mL (170.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 50 mg/mL (170.76 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (341.52 mM); Clear solution; Need ultrasonic
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 3.4152 mL | 17.0759 mL | 34.1518 mL | 85.3796 mL |
| 5 mM | 0.6830 mL | 3.4152 mL | 6.8304 mL | 17.0759 mL | |
| 10 mM | 0.3415 mL | 1.7076 mL | 3.4152 mL | 8.5380 mL | |
| 15 mM | 0.2277 mL | 1.1384 mL | 2.2768 mL | 5.6920 mL | |
| 20 mM | 0.1708 mL | 0.8538 mL | 1.7076 mL | 4.2690 mL | |
| 25 mM | 0.1366 mL | 0.6830 mL | 1.3661 mL | 3.4152 mL | |
| 30 mM | 0.1138 mL | 0.5692 mL | 1.1384 mL | 2.8460 mL | |
| 40 mM | 0.0854 mL | 0.4269 mL | 0.8538 mL | 2.1345 mL | |
| 50 mM | 0.0683 mL | 0.3415 mL | 0.6830 mL | 1.7076 mL | |
| 60 mM | 0.0569 mL | 0.2846 mL | 0.5692 mL | 1.4230 mL | |
| 80 mM | 0.0427 mL | 0.2134 mL | 0.4269 mL | 1.0672 mL | |
| 100 mM | 0.0342 mL | 0.1708 mL | 0.3415 mL | 0.8538 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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