Rivastigmine

Catalog No.S4687 Batch:S468701

Technical Data

Formula	C₁₄H₂₂N₂O₂
Molecular Weight	250.34	CAS No.	123441-03-2
Solubility (25°C)*	In vitro


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Biological Activity

Description

Rivastigmine (SDZ-ENA 713, Exelon) is a cholinesterase inhibitor with IC50 of 5.5 μM. It inhibits acetylcholinesterase (IC50 = 4.15 µM) and butyrylcholinesterase (IC50 = 37 nM).

Targets

cholinesterase ^[1]

In vivo

Preclinical biochemical studies indicates that rivastigmine has central nervous system selectivity over peripheral inhibition. It ameliorates memory impairment in rats with forebrain lesions. The drug is rapidly absorbed orally, with a bioavailability of 0.355 and low protein binding (40%). Its elimination halflife is less than 2 hours, and it is converted to an inactive metabolite at the site of action, bypassing hepatic metabolic pathways. Its disposition essentially is unaltered in patients with renal or hepatic impairment. It also has dosedependent effects on AChE inhibition^[1].

Density

1.038 g/mL

Protocol (from reference)

Cell Assay:^{^[3]}	Cell lines Human transfected conjunctival Chang P12 cells Concentrations various concentrations Incubation Time 7 days Method Chronic toxicity is assessed 7 days after continuous exposure of cells to donepezil or rivastigmine using cell viability and cell esterase activity and the estimated cell numbers as parameters for viability. Culture medium including the tested drugs is changed once after 4 days.
Animal Study:^{^[2]}	Animal Models Male Wistar albino rats Dosages 0.5, 1, 1.5 and 2.5 mg/kg Administration i.p.

Cell Assay:^{^[3]}

Cell lines
Human transfected conjunctival Chang P12 cells
Concentrations
various concentrations
Incubation Time
7 days
Method
Chronic toxicity is assessed 7 days after continuous exposure of cells to donepezil or rivastigmine using cell viability and cell esterase activity and the estimated cell numbers as parameters for viability. Culture medium including the tested drugs is changed once after 4 days.

Animal Study:^{^[2]}

Animal Models
Male Wistar albino rats
Dosages
0.5, 1, 1.5 and 2.5 mg/kg
Administration
i.p.

References

Selleck's Rivastigmine has been cited by 1 publication

Accumulation of 8,9-unsaturated sterols drives oligodendrocyte formation and remyelination [Hubler Z, et al. Nature, 2018, 560(7718):372-376]	PubMed: 30046109

Accumulation of 8,9-unsaturated sterols drives oligodendrocyte formation and remyelination [Hubler Z, et al. Nature, 2018, 560(7718):372-376]

PubMed: 30046109

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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