MedChemExpress LLC (MCE)

MedChemExpress - Model Rivastigmine tartrate - 129101-54-8

Rivastigmine tartrate (ENA 713; SDZ-ENA 713) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively. Rivastigmine tartrate can pass the blood brain barrier (BBB). Rivastigmine tartrate is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease[1][2].

Rivastigmine tartrate

MCE China：Rivastigmine tartrate

Brand：MedChemExpress (MCE)

Cat. No.HY-11017

CAS：129101-54-8

Synonyms：ENA 713; SDZ-ENA 713

Purity：99.03%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Rivastigmine tartrate (ENA 713; SDZ-ENA 713) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively. Rivastigmine tartrate can pass the blood brain barrier (BBB). Rivastigmine tartrate is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease.

In Vitro：Rivastigmine tartrate (ENA 713; 1 μM; 24 hours) reduces LPS (2.5 μg/ml)-induced TNF-α and IL-6 by 50% and 46% combined with carbachol (10 μM), respectively and does not cause any significant reduction in pro-inflammatory cytokines [3]. Rivastigmine tartrate (1 μM), carbachol (10 μM), or a combination of both drugs, does not have a cytotoxic effect on activated cells[3].

In Vivo：Rivastigmine tartrate (ENA 713; 0.5-2.5 mg/kg; IP; 60 min before the tests) significantly and dose-dependently improved the behavioral impairments caused by Aluminum (HY-B1521)[4]. Rivastigmine (0.5, 1 mg/kg/day; s.c; for 8 days) reduces by about 50% and 60% respectively, the concentration of IL-6 but not those of TNF-α and IL-1β in BALB/c OlaHsd male mice aged 8-9 weeks weighing 200–250 g with acute colitis[3]. Rivastigmine (1 mg/kg), but not (0.5 mg/kg), partially antagonized colon shrinkage and completely prevented bleeding. Treatment with rivastigmine (0.5 mg/kg) causes little change in these pathological manifestations, but rivastigmine (1 mg/kg) causes a partial restoration of the structure of the crypts and a reduction in sub-mucosal edema and cell infiltration. Rivastigmine (1 mg/kg) causes a 4.7% reduction in body weight at the end of the experiment[3].

IC50 & Target：AChE

References：

[1]. Qian-Sheng Yu, et al. Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines. J Med Chem. 2002 Aug 15;45(17):3684-91. [Content Brief]

[2]. Han HJ, Lee JJ, Park SA et al. Efficacy and safety of switching from oral cholinesterase inhibitors to the rivastigmine transdermal patch in patients with probable Alzheimer's disease. J Clin Neurol. 2011 Sep;7(3):137-42. [Content Brief]

[3]. Helena Shifrin, et al. Rivastigmine alleviates experimentally induced colitis in mice and rats by acting at central and peripheral sites to modulate immune responses. PLoS One. 2013;8(2):e57668. [Content Brief]

[4]. Raafat A Abdel-Aal, et al. Rivastigmine reverses aluminum-induced behavioral changes in rats. Eur J Pharmacol. 2011 Jun 1;659(2-3):169-76. [Content Brief]

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