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Mexiletine HCl

Na+ channel blocker; antiarrhythmic agent CAS# 5370-01-4

Mexiletine HCl

Catalog No. BCC4677----Order now to get a substantial discount!

Product Name & Size Price Stock
Mexiletine HCl:50mg $67.00 In stock
Mexiletine HCl:100mg $114.00 In stock
Mexiletine HCl:250mg $268.00 In stock
Mexiletine HCl:500mg $469.00 In stock
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Chemical structure

Mexiletine HCl

3D structure

Chemical Properties of Mexiletine HCl

Cas No. 5370-01-4 SDF Download SDF
PubChem ID 21467 Appearance Powder
Formula C11H18ClNO M.Wt 215.72
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Ko 1173
Solubility DMSO : ≥ 41 mg/mL (190.06 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 1-(2,6-Dimethylphenoxy)-2-propanamine hydrochloride
SMILES [H+].[Cl-].CC(N)COc1c(C)cccc1C
Standard InChIKey NFEIBWMZVIVJLQ-UHFFFAOYSA-N
Standard InChI InChI=1S/C11H17NO.ClH/c1-8-5-4-6-9(2)11(8)13-7-10(3)12;/h4-6,10H,7,12H2,1-3H3;1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Mexiletine HCl

DescriptionUse-dependent sodium channel blocker (IC50 values are 75.3 and 23.6 μM for tonic and use-dependent block respectively). Class Ib antiarrhythmic, neuroprotective and antimyotonic agent.

Mexiletine HCl Dilution Calculator

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Mexiletine HCl Molarity Calculator

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Preparing Stock Solutions of Mexiletine HCl

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 4.6356 mL 23.1782 mL 46.3564 mL 92.7128 mL 115.891 mL
5 mM 0.9271 mL 4.6356 mL 9.2713 mL 18.5426 mL 23.1782 mL
10 mM 0.4636 mL 2.3178 mL 4.6356 mL 9.2713 mL 11.5891 mL
50 mM 0.0927 mL 0.4636 mL 0.9271 mL 1.8543 mL 2.3178 mL
100 mM 0.0464 mL 0.2318 mL 0.4636 mL 0.9271 mL 1.1589 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Mexiletine HCl

Mexiletine HCl belongs to Class IB anti-arrhythmic group of medicines, inhibits sodium channels to reduce the inward sodium current.

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References on Mexiletine HCl

Neuroprotective effect of mexiletine in the central nervous system of diabetic rats.[Pubmed:16541198]

Mol Cell Biochem. 2006 Jun;286(1-2):125-31.

Both experimental and clinical studies suggests that oxidative stress plays an important role in the pathogenesis of diabetes mellitus type 1 and type 2. Hyperglycaemia leads to free radical generation and causes neural degeneration. In the present study we investigated the possible neuroprotective effect of mexiletine against streptozotocin-induced hyperglycaemia in the rat brain and spinal cord. 30 adult male Wistar rats were divided into three groups: control, diabetic, and diabetic-mexiletine treated group. Diabetes mellitus was induced by a single injection of streptozotocin (60 mg/kg body weight). Mexiletine (50 mg/kg) was injected intraperitoneally every day for six weeks. After 6 weeks the brain, brain stem and cervical spinal cord of the rats were removed and the hippocampus, cortex, cerebellum, brain stem and spinal cord were dissected for biochemical analysis (the level of Malondialdehide [MDA], Nitric Oxide [NO], Reduced Glutathione [GSH], and Xanthine Oxidase [XO] activity). MDA, XO and NO levels in the hippocampus, cortex, cerebellum, brain stem and spinal cord of the diabetic group increased significantly, when compared with control and mexiletine groups (P < 0.05). GSH levels in the hippocampus, cortex, cerebellum, brain stem and spinal cord of the diabetic group decreased significantly when compared with control and mexiletine groups (P < 0.05). This study demonstrates that mexiletine protects the neuronal tissue against the diabetic oxidative damage.

Evaluation of the pharmacological activity of the major mexiletine metabolites on skeletal muscle sodium currents.[Pubmed:16921388]

Br J Pharmacol. 2006 Oct;149(3):300-10.

BACKGROUND AND PURPOSE: Mexiletine (Mex), an orally effective antiarrhythmic agent used to treat ventricular arrhythmias, has also been found to be effective for myotonia and neuropathic pain. It is extensively metabolized in humans but little information exists about the pharmacodynamic properties of its metabolites. EXPERIMENTAL APPROACH: To determine their contribution to the clinical activity of Mex, p-hydroxy-mexiletine (PHM), hydroxy-methyl-mexiletine (HMM), N-hydroxy-mexiletine (NHM) (phase I reaction products) and N-carbonyloxy beta-D-glucuronide (NMG) (phase II reaction product) were tested on sodium currents (I(Na)) of frog skeletal muscle fibres. Sodium currents were elicited with depolarizing pulses from different holding potentials (HP=-140, -100, -70 mV) and stimulation frequencies (0.25, 0.5, 1, 2, 5, 10 Hz) using the vaseline-gap voltage-clamp method. KEY RESULTS: All the hydroxylated derivatives blocked the sodium channel in a voltage- and use-dependent manner. The PHM, HMM and NHM metabolites were up to 10-fold less effective than the parent compound. However, HMM showed a greater use-dependent behaviour (10 Hz), compared to Mex and the other metabolites. Similar to Mex, these products behaved as inactivating channel blockers. Conjugation with glucuronic acid (NMG) resulted in almost complete abolition of the pharmacological activity of the parent compound. CONCLUSIONS AND IMPLICATIONS: Thus, although less potent, the phase I metabolites tested demonstrated similar pharmacological behaviour to Mex and might contribute to its clinical profile.

Optically active mexiletine analogues as stereoselective blockers of voltage-gated Na(+) channels.[Pubmed:14613326]

J Med Chem. 2003 Nov 20;46(24):5238-48.

Optically active mexiletine analogues were synthesized and evaluated in vitro as use-dependent blockers of skeletal muscle sodium channels. The mexiletine analogues were obtained by replacing either the methyl group on the stereogenic center of mexiletine [1-(2,6-dimethylphenoxy)propan-2-amine] with a phenyl group or modifying the phenoxy moiety (by removal of one or both of the methyl groups, or introducing a chlorine atom), or both. The voltage clamp recordings showed that, regardless of the substitution pattern of the aryloxy moiety, all the compounds bearing a phenyl group on the stereogenic center (3a-f) were more active than mexiletine both in tonic and phasic block. This observation was in contrast with what was observed for mexiletine, where the removal of both methyls from the aryloxy moiety caused a dramatic reduction of potency. The most potent congener, (R)-2-(2-methylphenoxy)-1-phenylethanamine [(R)-3b], was 27-fold more potent than (R)-mexiletine in producing a tonic block, i.e., the reduction of peak sodium current in resting conditions after application of the compound. (R)-3b maintained a use-dependent behavior, being 23-fold more potent in condition of high frequency of stimulation (phasic block). Despite what was observed with mexiletine, the stereoselectivity held in phasic block conditions. Stereoselectivity indexes were generally low, ranging from 1 to 4, but except for that of the 2,6-xylyloxy congener 3c, they were higher for the congeners bearing a phenyl ring on the stereogenic center than for mexiletine and its strictly related analogue 1-methyl-2-phenoxyethanamine (1). This finding was in agreement with Pfeiffer's rule. The introduction of a chlorine atom in the 4-position of the aryloxy moiety caused a reduction of potency and a reversal of stereoselectivity as well. On the basis of the model to date accepted for the sodium channel local anesthetic-like molecule receptor, some possible explanations of our observations will be proposed.

Description

Mexiletine hydrochloride (KOE-1173 hydrochloride), a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker.

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