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[CAS NO. 58337-38-5] EHNA hydrochloride
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-103160A |
| Brand: | MCE |
| CAS: | 58337-38-5 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 313.83 |
| Molecular Formula | C14H24ClN5O |
| SMILES | CCCCCC[C@@](N1C2=C(C(N)=NC=N2)N=C1)([H])[C@H](O)C.[Relative stereochemistry].Cl |
3 Publications Citing Use of MCE
Summary
EHNA hydrochloride is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2) ( IC 50 =4 μM) and adenosine deaminase (ADA) . EHNA hydrochloride exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)( IC 50 :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 [1] [2] .
IC50 & Target
|
hPDE2A 0.8 μM (IC 50 ) |
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : ≥ 250 mg/mL ( 796.61 mM )
H 2 O : 100 mg/mL ( 318.64 mM ; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.1864 mL | 15.9322 mL | 31.8644 mL |
| 5 mM | 0.6373 mL | 3.1864 mL | 6.3729 mL |
| 10 mM | 0.3186 mL | 1.5932 mL | 3.1864 mL |
References
- [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.
- [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.
- [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.
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