1. Neuronal Signaling
  2. Cholinesterase (ChE)
  3. Rivastigmine

Rivastigmine  (Synonyms: ENA 713 free base; SDZ-ENA 713 free base)

Cat. No.: HY-17368 Purity: 99.93%
COA Handling Instructions

Rivastigmine (ENA 713 free base) 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 can pass the blood brain barrier (BBB). Rivastigmine 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 Chemical Structure

Rivastigmine Chemical Structure

CAS No. : 123441-03-2

Size Price Stock Quantity
Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 87 In-stock
Solution
10 mM * 1 mL in DMSO USD 87 In-stock
Liquid
50 mg USD 79 In-stock
100 mg USD 119 In-stock
200 mg USD 158 In-stock
500 mg USD 198 In-stock
1 g   Get quote  
5 g   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Rivastigmine:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Rivastigmine

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Rivastigmine (ENA 713 free base) 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 can pass the blood brain barrier (BBB). Rivastigmine 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

AChE

 

BChE

 

In Vitro

Rivastigmine (ENA 713 free base; 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 (1 μM), carbachol (10 μM), or a combination of both drugs, does not have a cytotoxic effect on activated cells[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Rivastigmine (ENA 713 free base; 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

250.34

Formula

C14H22N2O2

CAS No.
Appearance

Liquid (Density: 1.038±0.06 g/cm3)

Color

Colorless to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : ≥ 50 mg/mL (199.73 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9946 mL 19.9728 mL 39.9457 mL
5 mM 0.7989 mL 3.9946 mL 7.9891 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.93%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.9946 mL 19.9728 mL 39.9457 mL 99.8642 mL
5 mM 0.7989 mL 3.9946 mL 7.9891 mL 19.9728 mL
10 mM 0.3995 mL 1.9973 mL 3.9946 mL 9.9864 mL
15 mM 0.2663 mL 1.3315 mL 2.6630 mL 6.6576 mL
20 mM 0.1997 mL 0.9986 mL 1.9973 mL 4.9932 mL
25 mM 0.1598 mL 0.7989 mL 1.5978 mL 3.9946 mL
30 mM 0.1332 mL 0.6658 mL 1.3315 mL 3.3288 mL
40 mM 0.0999 mL 0.4993 mL 0.9986 mL 2.4966 mL
50 mM 0.0799 mL 0.3995 mL 0.7989 mL 1.9973 mL
60 mM 0.0666 mL 0.3329 mL 0.6658 mL 1.6644 mL
80 mM 0.0499 mL 0.2497 mL 0.4993 mL 1.2483 mL
100 mM 0.0399 mL 0.1997 mL 0.3995 mL 0.9986 mL
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Rivastigmine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Rivastigmine
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