product name Mexiletine HCl
Description: Mexiletine HCl (also known as KO1173) belongs to Class IB anti-arrhythmic group of medicines, it inhibits sodium channels to reduce the inward sodium current. Mexiletine is a local anesthetic, antiarrhythmic agent (Class Ib), structurally similar to lidocaine, but orally active. Mexiletine, inhibits the inward sodium current required for the initiation and conduction of impulses, thus reducing the rate of rise of the action potential. It achieves this reduced sodium current by inhibiting sodium channels.
References:Curr Med Chem. 2015;22(11):1400-13; Curr Pain Headache Rep. 2010 Apr;14(2):145-50.
215.72
Formula
C11H17NO.HCl
CAS No.
5370-01-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 43 mg/mL (199.3 mM)
Water: 43 mg/mL (199.3 mM)
Ethanol: 43 mg/mL (199.3 mM)
Solubility (In vivo)
Synonyms
KO1173
other peoduct :
| In Vitro |
In vitro activity: Mexiletine is a local anesthetic, antiarrhythmic agent (Class Ib), structurally similar to lidocaine, but orally active. Mexiletine, inhibits the inward sodium current required for the initiation and conduction of impulses, thus reducing the rate of rise of the action potential. It achieves this reduced sodium current by inhibiting sodium channels. Mexiletine decreases the effective refractory period (ERP) in Purkinje fibers in the heart. The decrease in ERP is of lesser magnitude than the decrease in action potential duration (APD), which results in an increase in the ERP/APD ratio. It does not significantly affect resting membrane potential or sinus node automaticity, left ventricular function, systolic arterial blood pressure, atrioventricular (AV) conduction velocity, or QRS or QT intervals Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Mexiletine has fast onset and offset kinetics, meaning that they have little or no effect at slower heart rates, and more effects at faster heart rates. It shortens the action potential duration, reduces refractoriness, and decreases Vmax in partially depolarized cells with fast response action potentials. Mexiletine either does not change the action potential duration, or decreases the action potential duration. Mexiletine is well absorbed (bioavailability 90%) from the gastrointenstinal tract. |
| Animal model | |
| Formulation & Dosage | |
| References | Curr Med Chem. 2015;22(11):1400-13; Curr Pain Headache Rep. 2010 Apr;14(2):145-50. |
