1. Neuronal Signaling
  2. AChE
  3. Rivastigmine tartrate

Rivastigmine tartrate (Synonyms: ENA 713; SDZ-ENA 713)

Cat. No.: HY-11017 Purity: 99.45%
Handling Instructions

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.

For research use only. We do not sell to patients.

Rivastigmine tartrate Chemical Structure

Rivastigmine tartrate Chemical Structure

CAS No. : 129101-54-8

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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[1][2].

IC50 & Target

IC50: 0.037 μM (BChE) and 4.15 μM (AChE)[1]

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].

Animal Model: Male Wistar albino rats weighing 190–240 g (90 days old)[4]
Dosage: 0.5, 1, 1.5 and 2.5 mg/kg
Administration: IP; single dose
Result: Significantly and dose-dependently improved the behavioral impairments caused by Aluminum (100 mg/kg/day; i.p.; for 60 days)
Clinical Trial
Molecular Weight

400.42

Formula

C₁₈H₂₈N₂O₈

CAS No.

129101-54-8

SMILES

O=C(OC1=CC=CC([[email protected]@H](N(C)C)C)=C1)N(CC)C.O=C(O)[[email protected]](O)[[email protected]@H](O)C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (124.87 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4974 mL 12.4869 mL 24.9738 mL
5 mM 0.4995 mL 2.4974 mL 4.9948 mL
10 mM 0.2497 mL 1.2487 mL 2.4974 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

RivastigmineENA 713 SDZ-ENA 713ENA713ENA-713AChEAcetylcholinesteraseorallycholinesteraseChEbutyrylcholinesteraseBChEacetylcholinesterasparasympathomimeticcholinergicAlzheimer'sParkinson'sdiseaseBBBInhibitorinhibitorinhibit

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Rivastigmine tartrate
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