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Recent large clinical trials failed to confirm the supposed beneficial effects of N-acetylcysteine (NAC) in preventing oxidative stress-related diseases. This may be due to its low bioavailability. We thought that esterification of the carboxyl group of NAC to produce N-acetylcysteine ethyl ester (NACET) would drastically increase the lipophilicity of NAC, thus greatly improving its pharmacokinetics. In the present work, we report on representative chemical, pharmacological and anti-oxidant properties of NACET, especially in direct comparison with its congener NAC. We found that NACET is rapidly absorbed in rats after oral administration but reaches very low concentrations in plasma. This is due to a unique feature of NACET: it rapidly enters the cells where it is trapped being transformed into NAC and cysteine. After oral treatment, NACET (but not NAC) was able to increase significantly the glutathione content of most tissues examined, brain included, and to protect from paracetamol intoxication in the rat.
The esterification of the carboxyl group to produce N-acetylcysteine ethyl ester increases the lipophilicity of NAC and greatly improves its pharmacokinetics. NACET has much higher bioavailability (around 60%) than NAC. NACET rapidly enters the cells, then is trapped, and transforms into NAC and Cysteine. NACET is found in the cells of different tissues, including brain as it is able to cross the blood-brain barrier. NACET also provides a variety of protective antioxidant effects. NACET may be taken orally and helps increase glutathione. It can accumulate in human erythrocytes. NACET may also behave as a potent protector against hydroperoxide-induced oxidative damage. NACA has superior bioavailability than NAC as well as a molecule to improve the endurance and resident time of bioscaffolds and biomaterials. More than 800 reviews on NAC have been published.
General population:
50mg-100mg
Adults:
50mg-100mg
Ideal for:
Up to one week for full effects to manifest. Best combined with Glycine.
Brain Health, Neural restoration, students, athletes.
Based on NAC strong safety profile, this compound is likely also safe, however, literature reviews are pending.
Not available.
The esterification of the carboxyl group to produce N-acetylcysteine ethyl ester increases the lipophilicity of NAC and greatly improves its pharmacokinetics. NACET has much higher bioavailability (around 60%) than NAC. NACET rapidly enters the cells, then is trapped, and transforms into NAC and Cysteine. NACET is found in the cells of different tissues, including brain as it is able to cross the blood-brain barrier. NACET also provides a variety of protective antioxidant effects. NACET may be taken orally and helps increase glutathione. It can accumulate in human erythrocytes. NACET may also behave as a potent protector against hydroperoxide-induced oxidative damage. NACA has superior bioavailability than NAC as well as a molecule to improve the endurance and resident time of bioscaffolds and biomaterials. More than 800 reviews on NAC have been published.
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NACET has far superior effects over regular NAC, with a lower dosage needed. It is going to be hot in the next couple of years.
