| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C14H24ClN5O |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
EHNA hydrochloride is a potent, selective, dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2, IC50 = 4 μM) and adenosine deaminase (ADA). It inhibits cGMP-stimulated PDE II (cGs-PDE) in a concentration-dependent manner, with IC50 values of 0.8 μM in human and 2 μM in porcine myocardium, but has a smaller inhibitory effect on unstimulated PDE2 activity. It plays roles in mediating diverse pharmacological responses, including antiviral, antitumor, and antiarrhythmic effects[1][2]. It is supplied as a white to light yellow solid (C14H24ClN5O, MW 313.83) at 99.67% purity.
Physical & Chemical Properties
| CAS Number | 58337-38-5 |
|---|---|
| Molecular Formula | C14H24ClN5O |
| Molecular Weight | 313.83 g/mol |
| Purity | 99.67% |
| Appearance | Solid |
| Color | White to light yellow |
| SMILES | CCCCCC[C@@](N1C2=C(C(N)=NC=N2)N=C1)([H])[C@H](O)C.Cl |
| Target | PDE2, hPDE2A |
| Signaling Pathway | Metabolic Enzyme/Protease; Anti-infection |
| Solubility | In Vitro: H2O: 100 mg/mL (318.64 mM; Requires sonication) DMSO: 83.33 mg/mL (265.53 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | -20°C, sealed storage, away from moisture. In solvent: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
hPDE2A 0.8 μM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| H2O | 100 mg/mL (318.64 mM) | requires sonication |
| DMSO | 83.33 mg/mL (265.53 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (6.63 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.08 mg/mL (6.63 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.08 mg/mL (6.63 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
EHNA completely abolishes the capacity of cyclic GMP to activate PDE2 activity, with a much smaller inhibitory effect on unstimulated PDE2 activity[2]. Inhibition of cyclic GMP-stimulated PDE2 activity by EHNA follows normal Michaelian kinetics, with Hill plots near unity[2]. In fibroblasts, EHNA prevents dAdo degradation and raises mitochondrial dATP levels[3].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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