| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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ZD7288 (ZD-7288; ZD 7288) is a novel and potent sino-atrial node function modulator that blocks the hyperpolarization activated cation current If (HCN channel). It also blocks Ih in central neurons and increases NMDA-evoked noradrenalin release in rat brain in vitro.
| ln Vitro |
ZD7288 functions as an activating ring-labeled gated (HCN) channel blocker, both transient and ultra-transient. Glutathione release is inhibited by ZD7288 in a concentration-inhibitory way. Following a 24-hour buffering period with 1, 5, and 50 μM ZD7288, the extracellular fluid's glutamate level dropped to 69.0±2.8%, 31.4±2.0%, and 4.4±0.3%, respectively (P<0.01, when compared to the DMEM/F12 group Ratio [100.2±4.2%]). Once ZD7288 (25) amino acids were added for 20 minutes, the [Ca2+]i generated by 50 μM glutamate increased to 59.2±2.7%, 41.4±2.3%, and 21.0±1.4% for glutamate, respectively (P <0.01, in comparison to the 50 μM glutamate group)[1].
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| ln Vivo |
The amplitude of field excitatory postsynaptic potentials (fEPSP) was dramatically reduced when ZD7288 0.1 μM was applied five minutes before to high-frequency stimulation. This inhibitory effect persisted for the duration of the recording. Thirty minutes after high-frequency stimulation, application of 0.1 μM ZD7288 nearly reversed established long-term potentiation (LTP). Five minutes prior to high-frequency stimulation, ZD7288 (0.1 μM) application resulted in a 74.9±8.0% (P<0.05) reduction in glutamate content when compared to the normal saline group. Furthermore, 30 minutes following high-frequency stimulation, applying 0.1 μM ZD7288 could dramatically lower glutamic acid concentration, which reached 77.0%±9.4% (P<0.05) when compared to the normal saline group [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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| Molecular Formula |
C15H20N4
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|---|---|
| Molecular Weight |
256.35
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| Exact Mass |
256.1688
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| CAS # |
133059-99-1
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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 |
ZD 7288 ZD-7288 ZD7288
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~170.76 mM)
H2O : ≥ 50 mg/mL (~170.76 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (341.52 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9009 mL | 19.5046 mL | 39.0092 mL | |
| 5 mM | 0.7802 mL | 3.9009 mL | 7.8018 mL | |
| 10 mM | 0.3901 mL | 1.9505 mL | 3.9009 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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