1. Membrane Transporter/Ion Channel
  2. HCN Channel

ZD7288 (Synonyms: ICI D7288)

Cat. No.: HY-101346 Purity: 99.79%
Handling Instructions

ZD7288 is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker.

For research use only. We do not sell to patients.

ZD7288 Chemical Structure

ZD7288 Chemical Structure

CAS No. : 133059-99-1

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10 mM * 1 mL in Water USD 110 In-stock
Estimated Time of Arrival: December 31
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Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

ZD7288 is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker.

IC50 & Target

HCN channel[1]

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 [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].

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)[1].

Solvent & Solubility
In Vitro: 

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

H2O : ≥ 50 mg/mL (170.76 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

292.81

Formula

C₁₅H₂₁ClN₄

CAS No.

133059-99-1

SMILES

[H]Cl.C/N=C1C=C(N(CC)C2=CC=CC=C2)N=C(C)N/1C

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
ZD7288
Cat. No.:
HY-101346
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ZD7288

Cat. No.: HY-101346