[CAS NO. 58337-38-5]  EHNA hydrochloride

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PRODUCTS SPECIFICATIONS [58337-38-5]

Catalog
HY-103160A
Brand
MCE
CAS
58337-38-5

DESCRIPTION [58337-38-5]

Overview

MDL-
Molecular Weight313.83
Molecular FormulaC14H24ClN5O
SMILESCCCCCC[C@@](N1C2=C(C(N)=NC=N2)N=C1)([H])[C@H](O)C.[Relative stereochemistry].Cl

For research use only. We do not sell to patients.


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

In Vitro:

DMSO : ≥ 250 mg/mL ( 796.61 mM )

H 2 O : 100 mg/mL ( 318.64 mM ; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

Preparing
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
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.63 mM); Clear solution

* All of the co-solvents are available by MCE.