EHNA hydrochloride
Based on 5 publication(s) in Google Scholar
EHNA hydrochloride is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA hydrochloride exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA hydrochloride play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects.
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- Pureza: 99.67%
- No. CAS: 58337-38-5
- Fòrmula: C14H24ClN5O
- Peso molecular:313.83
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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EHNA hydrochloride (Standard) -
HY-12318
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Publications Citing Use of MedChemExpress (MCE) EHNA hydrochloride
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PK/PD Analysis
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PK/PD Analysis
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Cell Proliferation/Viability Assay
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
Actividad biológica
Descripciòn
IC50 & Target
[1]|
PDE2 |
hPDE2A 0.8 μM (IC50) |
In Vitro
EHNA completely ablates the ability of cyclic GMP to activate PDE2 activity, whilst having a much smaller inhibitory effect on the unstimulated PDE2 activity[2].EHNA exhibits normal Michaelian kinetics of inhibition for the cyclic GMP-stimulated PDE2 activity with Hill plots near unity[2].EHNA prevents dAdo degradation and increases mitochondrial dATP levels in fibroblasts[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 58337-38-5
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Appearance Solid
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Peso molecular 313.83
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Fòrmula C14H24ClN5O
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Color White to light yellow
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SMILES
CCCCCC[C@@](N1C2=C(C(N)=NC=N2)N=C1)([H])[C@H](O)C.Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (5)
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Journal Impact Factor
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Most Recent
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Nucleic Acids Res
Metabolic isotopic labeling of (deoxy)ribose enables dual neutral loss scanning for profiling nucleic acid modifications. [Abstract]2026 Feb 24;54(5):gkag155. PMID: 41732913 -
Front Immunol
CD38+CD39+ NK cells associate with HIV disease progression and negatively regulate T cell proliferation. [Abstract]2022 Oct 4:13:946871. PMID: 36268017
EHNA hydrochloride purchased from MedChemExpress. Usage Cited in: Front Immunol. 2022 Oct 4:13:946871. [Abstract]
EHNA hydrochloride (100 μM; 30 min)-mediated inhibition of adenosine deaminase (ADA) impairs the proliferation of CD4+ T cells, whereas CD8+ T cell proliferation remains unaffected.
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Oncoimmunology
Overcoming the resistance of hepatocellular carcinoma to PD-1/PD-L1 inhibitor and the resultant immunosuppression by CD38 siRNA-loaded extracellular vesicles. [Abstract]2022 Dec 26;12(1):2152635. PMID: 36605619
EHNA hydrochloride purchased from MedChemExpress. Usage Cited in: Oncoimmunology. 2022 Dec 26;12(1):2152635. [Abstract]
Adenosine production in HCCLM3 cells. The results showed that Culture medium of siNC- and siCD38-treated HCCLM3 cells without EHNA hydrochloride (100 μM) intervention showed gradually degraded adenosine and no accumulation, with no significant difference, while upon EHNA hydrochloride, adenosine accumulated in the medium and its content was decreased in response to siCD38 at different time points (6 h, 12 h, 18 h, and 24 h).
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Eur J Pharmacol
Bay 60-7550, a PDE2 inhibitor, exerts positive inotropic effect of rat heart by increasing PKA-mediated phosphorylation of phospholamban. [Abstract]2021 Jun 15:901:174077. PMID: 33798601
EHNA hydrochloride purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2021 Jun 15:901:174077. [Abstract]
The effects of EHNA hydrochloride (0.01, 0.1, 1, 10 μmol/L) were also presented in non-pacing and pacing modes in ex vivo isolated rat left hearts. EHNA: a classical PDE2 inhibitor. During the experiments, these different concentrations of EHNA from low to high concentration order were added to the perfusion solution and infused via retrograde perfusion of the coronary artery. The hemodynamic parameters were recorded when isolated heart contraction reached constant level with EHNA perfusions longer than 10 min for each concentration. Their intraventricular pressures were measured.
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Biomed Chromatogr
Distribution and Pharmacokinetic Characteristics of Cordycepin in Rat: Investigated by UHPLC-HRMS/MS and Blood-Brain Synchronous Microdialysis. [Abstract]2025 Apr;39(4):e70038. PMID: 40071940
EHNA hydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Chromatogr. 2025 Apr;39(4):e70038. [Abstract]
Time-course curves of cordycepin in rat blood and brain after administration of cordycepin (10 mg/kg; i.p.) with EHNA hydrochloride (10 mg/kg; i.p.; single dose).
EHNA hydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Chromatogr. 2025 Apr;39(4):e70038. [Abstract]
Time-course curves of 3′-deoxyinosine in rat blood and brain after administration of cordycepin (10 mg/kg; i.p.) with or without EHNA hydrochloride (10 mg/kg; i.p.; single dose).
Solvente y solubilidad
In Vitro:
H2O : 100 mg/mL (318.64 mM; Need ultrasonic)
DMSO : 83.33 mg/mL (265.53 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* 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.
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.63 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.63 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Podzuweit T, et al. Isozyme selective inhibition of cGMP-stimulated cyclic nucleotide phosphodiesterases by erythro-9-(2-hydroxy-3-nonyl) adenine.Cell Signal. 1995 Sep;7(7):733-8. [Content Brief]
[2]. Michie AM, et al. Rapid regulation of PDE-2 and PDE-4 cyclic AMP phosphodiesterase activity following ligation of the T cell antigen receptor on thymocytes: analysis using the selective inhibitors erythro-9-(2-hydroxy-3-nonyl)-adenine (EHNA) and rolipram.Cell Signal. 1996 Feb;8(2):97-110. [Content Brief]
[3]. Blázquez-Bermejo C, et al. Increased dNTP pools rescue mtDNA depletion in human POLG-deficient fibroblasts. FASEB J. 2019 Jun;33(6):7168-7179. [Content Brief]
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 3.1864 mL | 15.9322 mL | 31.8644 mL | 79.6610 mL |
| 5 mM | 0.6373 mL | 3.1864 mL | 6.3729 mL | 15.9322 mL | |
| 10 mM | 0.3186 mL | 1.5932 mL | 3.1864 mL | 7.9661 mL | |
| 15 mM | 0.2124 mL | 1.0621 mL | 2.1243 mL | 5.3107 mL | |
| 20 mM | 0.1593 mL | 0.7966 mL | 1.5932 mL | 3.9830 mL | |
| 25 mM | 0.1275 mL | 0.6373 mL | 1.2746 mL | 3.1864 mL | |
| 30 mM | 0.1062 mL | 0.5311 mL | 1.0621 mL | 2.6554 mL | |
| 40 mM | 0.0797 mL | 0.3983 mL | 0.7966 mL | 1.9915 mL | |
| 50 mM | 0.0637 mL | 0.3186 mL | 0.6373 mL | 1.5932 mL | |
| 60 mM | 0.0531 mL | 0.2655 mL | 0.5311 mL | 1.3277 mL | |
| 80 mM | 0.0398 mL | 0.1992 mL | 0.3983 mL | 0.9958 mL | |
| 100 mM | 0.0319 mL | 0.1593 mL | 0.3186 mL | 0.7966 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.
EHNA hydrochloride Related Classifications
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