2. Membrane Transporter/Ion Channel
  3. HCN Channel
  4. ZD7288

ZD7288 (ICI D7288) is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker.

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No. CAS : 133059-99-1

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10 mM * 1 mL in DMSO
ready for reconstitution
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Revisión del cliente

Based on 9 publication(s) in Google Scholar

Other Forms of ZD7288:

ZD7288 Related Antibodies

Top Publications Citing Use of Products

    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.

    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.

    • Actividad biológica

    • Protocolo

    • Pureza y Documentación

    • Referencias

    • Revisión del cliente

    Descripciòn

    ZD7288 (ICI D7288) is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker[1].

    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].

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

    ZD7288 Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Peso molecular

    292.81

    Fòrmula

    C15H21ClN4
    No. CAS
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Almacenamiento

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvente y solubilidad
    In Vitro: 

    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.

    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
    View the 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.

    * 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.

    • Calculadora de molaridad

    • Calculadora de dilución

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 100 mg/mL (341.52 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Pureza y Documentación
    Referencias
    Ensayo celular
    [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 no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
    Administraciòn de animales
    [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 no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
    Referencias

    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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    ZD7288 Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    ZD7288133059-99-1ICI D7288ZD 7288ZD-7288ICI D 7288ICI D-7288HCN ChannelHyperpolarization activated cyclic nucleotide gated channelsInhibitorinhibitorinhibit

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