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

リバスチグミン  (Synonyms: Rivastigmine; S-Rivastigmine)

製品番号: HY-17368 純度: 99.95%
COA 取扱説明書 Technical Support

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.

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Rivastigmine

リバスチグミン 構造式

CAS 番号 : 123441-03-2

容量 価格(税別) 在庫状況 数量
Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 86 在庫あり
Solution
10 mM * 1 mL in DMSO USD 86 在庫あり
Liquid
50 mg $79 在庫あり
100 mg $119 在庫あり
200 mg $158 在庫あり
500 mg $198 在庫あり
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カスタマーレビュー

Based on 1 publication(s) in Google Scholar

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Cholinesterase (ChE) アイソフォーム固有の製品をすべて表示:

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製品説明

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

 

Cellular Effect
Cell Line Type Value Description References
SH-SY5Y CC50
67.82 μM
Compound: Rivastigmine
Cytotoxicity in human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs incubation by MTT assay
Cytotoxicity in human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs incubation by MTT assay
[PMID: 30822710]
体外実験

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.

体内実験

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)
分子量

250.34

分子式

C14H22N2O2

CAS 番号
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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Pure form -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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
10 mM 0.3995 mL 1.9973 mL 3.9946 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)

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Volume
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Molecular Weight *

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

×
体積 (開始)

V1

=
濃度 (終了)

C2

×
体積 (終了)

V2

体内:

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.
純度とドキュメンテーション

純度: 99.95%

参考文献

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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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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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製品名:
Rivastigmine
製品番号:
HY-17368
数量:
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