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M2727

Sigma-Aldrich

Mexiletine hydrochloride

≥98% (GC), powder, sodium channel blocker

Sinonimo/i:

1-(2,6-Dimethylphenoxy)-2-propanamine hydrochloride, 1-(2,6-Xylyloxy)-2-aminopropane hydrochloride

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About This Item

Formula empirica (notazione di Hill):
C11H17NO · HCl
Numero CAS:
5370-01-4
Peso molecolare:
215.72
Numero CE:
250-825-7
Numero MDL:
MFCD00216024
Codice UNSPSC:
12352200
ID PubChem:
24278542
NACRES:
NA.77

Nome del prodotto

Mexiletine hydrochloride, powder

Saggio

≥98% (GC)

Livello qualitativo

200

Stato

powder

Colore

white to off-white

Solubilità

methanol: 50 mg/mL

Ideatore

Boehringer Ingelheim

Temperatura di conservazione

2-8°C

Stringa SMILE

Cl[H].CC(N)COc1c(C)cccc1C

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
NFEIBWMZVIVJLQ-UHFFFAOYSA-N

Informazioni sul gene

human ... SCN10A(6336) , SCN11A(11280) , SCN1A(6323) , SCN2A(6326) , SCN3A(6328) , SCN4A(6329) , SCN5A(6331) , SCN7A(6332) , SCN8A(6334) , SCN9A(6335)

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Descrizione generale

Mexiletine is a class I B antiarrhythmic and an analog of lidocaine. It has shelf life of 10-12 hours and is metabolized in liver and eliminated post reduction, oxidation deamination or conjugation.

Applicazioni

Mexiletine hydrochloride has been used as a sodium channel blocker:
  • expressed in chinese hamster ovary cells
  • in human embryonic kidney (HEK) cells for whole cell patch-clamp studies
  • electrophysiology studies in HEK cells expressing Nav1.7 protein

Azioni biochim/fisiol

Mexiletine is a potent sodium channel blocker. It is a cardiac antiarrhythmic and is used as an adjuvant in headache and neuropathic pain Mexiletine is used for treating myotonia in sodium channelopathies and reduces the cardiac action potential depolarization but shows no impact on atrial refractoriness. Its inhibitory effect on sodium channels is effective in treating potassium aggravated myotonia.

Caratteristiche e vantaggi

This compound was developed by Boehringer Ingelheim. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Pittogrammi

Exclamation mark
GHS07

Avvertenze

Warning

Indicazioni di pericolo

H302

Classi di pericolo

Acute Tox. 4 Oral

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

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Certificati d'analisi (COA)

Lot/Batch Number
BCCB6374
BCBL6076V
BCBL6076
BCBL3766
011M1248V

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USP

USP

1598744

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USP

1134120

Cisapride

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D2920000

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Arnold E Pfahnl et al.
Heart rhythm, 4(1), 46-53 (2007-01-03)
Brugada and long QT type 3 syndromes are linked to sodium channel mutations and clinically cause arrhythmias that lead to sudden death. We have identified a novel threonine-to-isoleucine missense mutation at position 353 (T353I) adjacent to the pore-lining region of
K Mori et al.
Naunyn-Schmiedeberg's archives of pharmacology, 358(6), 641-648 (1999-01-08)
Recently we have reported that class III antiarrhythmic drugs including amiodarone inhibit the Na+-activated K+ (KNa) channels in isolated cardiac cells. In this study effects of antiarrhythmic drugs having class I and/or IV properties on the single KNa channel current
S Sicouri et al.
Journal of cardiovascular electrophysiology, 8(11), 1280-1290 (1997-12-12)
Recent clinical studies have reported a greater effectiveness of sodium channel block with mexiletine to abbreviate the QT interval in patients with the chromosome 3 variant (SCN5A, LQT3) of the long QT syndrome (LQTS) than those with the chromosome 7
E L Logigian et al.
Neurology, 74(18), 1441-1448 (2010-05-05)
To determine if mexiletine is safe and effective in reducing myotonia in myotonic dystrophy type 1 (DM1). Myotonia is an early, prominent symptom in DM1 and contributes to decreased dexterity, gait instability, difficulty with speech/swallowing, and muscle pain. A few
J F Desaphy et al.
Neuromuscular disorders : NMD, 9(3), 182-189 (1999-06-26)
The sea anemone toxin ATX II impairs skeletal muscle sodium channel inactivation, mimicking the persistent inward current observed in patients suffering from sodium channel myotonia. Mexiletine has beneficial effects on myotonia. To verify the efficiency of the drug on persistent
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