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ZD7288

Alias: ZD 7288 ZD-7288 ZD7288
Cat No.:V16699 Purity: ≥98%
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).
ZD7288
ZD7288 Chemical Structure CAS No.: 133059-99-1
Product category: HCN Channel
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
25mg
50mg
100mg
250mg
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Product Description

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.

Biological Activity I Assay Protocols (From Reference)
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].
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].
References

[1]. ZD7288, a selective hyperpolarization-activated cyclic nucleotide-gated channel blocker, inhibits hippocampal synaptic plasticity. Neural Regen Res. 2016 May;11(5):779-86.

Additional Infomation
4-(N-Ethyl-N-phenylamino)-1,2-dimethyl-6-(methylamino)pyrimidinium chloride is an organic molecular entity.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C15H20N4
Molecular Weight
256.35
Exact Mass
292.145
CAS #
133059-99-1
PubChem CID
123983
Appearance
White to off-white solid powder
Boiling Point
359.9ºC at 760 mmHg
Flash Point
171.4ºC
Vapour Pressure
2.31E-05mmHg at 25°C
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
3
Heavy Atom Count
20
Complexity
402
Defined Atom Stereocenter Count
0
InChi Key
DUWKUHWHTPRMAP-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H20N4.ClH/c1-5-19(13-9-7-6-8-10-13)15-11-14(16-3)18(4)12(2)17-15;/h6-11H,5H2,1-4H3;1H
Chemical Name
N-ethyl-1,2-dimethyl-6-methylimino-N-phenylpyrimidin-4-amine;hydrochloride
Synonyms
ZD 7288 ZD-7288 ZD7288
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~50 mg/mL (~170.76 mM)
H2O : ≥ 50 mg/mL (~170.76 mM)
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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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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