2. Neuronal Signaling
  3. Cholinesterase (ChE)
  4. Physostigmine

Physostigmine  (Synonyms: Eserine)

製品番号: HY-N6608 純度: 99.89%
COA 取扱説明書 Technical Support

Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning.

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Physostigmine

Physostigmine 構造式

CAS 番号 : 57-47-6

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 632 在庫あり
Solution
10 mM * 1 mL in DMSO USD 632 在庫あり
Solid
1 mg $230 在庫あり
5 mg $575 在庫あり
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Based on 2 publication(s) in Google Scholar

Other Forms of Physostigmine:

Physostigmine 関連抗体

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

すべてのアイソフォームを表示
AChE BChE

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製品説明

Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning[1][2][3][4].

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.16 μM
Compound: Eserine
Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 5 mins before substrate addition measured after 10 mins by Ellman's method
Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 5 mins before substrate addition measured after 10 mins by Ellman's method
10.1039/C1MD00221J
Sf21 IC50
> 1000 μM
Compound: Physostigmine
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
[PMID: 21965623]
Sf21 IC50
> 1000 μM
Compound: Physostigmine
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
[PMID: 21965623]
体内実験

Physostigmine (Eserine; 0.03-0.3 mg/kg; s.c.; daily for 6 weeks) improves deficits in contextual and cued memory in Tg(+) mice[2].
Physostigmine (IV; 0.1, 0.2 mg/kg) delays time to emergence from isoflurane anesthesia at doses ≥0.2 mg/kg in male Sprague-Dawley rats[4].

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

Animal Model: Heterozygous transgenic mice (Tg(+) mice)[2]
Dosage: 0.03, 0.1, and 0.3 mg/kg
Administration: SC; daily for 6 weeks
Result: Tended to normalize the contextual memory deficit in Tg(+) animals so that they became more similar to Tg(-) animals.
分子量

275.35

分子式

C15H21N3O2
CAS 番号
Appearance

Solid

Color

Light yellow to brown

SMILES

CN1[C@](N(C)CC2)([H])[C@]2(C)C3=C1C=CC(OC(NC)=O)=C3
Structure Classification
Initial Source
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -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 (181.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6317 mL 18.1587 mL 36.3174 mL
5 mM 0.7263 mL 3.6317 mL 7.2635 mL
10 mM 0.3632 mL 1.8159 mL 3.6317 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
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Concentration
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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

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体積 （終了）

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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: ≥ 2.08 mg/mL (7.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (7.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 99.92%

COA (251 KB) HNMR (467 KB) LCMS (94 KB)

取扱説明書 (2659 KB)
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 3.6317 mL 18.1587 mL 36.3174 mL 90.7935 mL
5 mM 0.7263 mL 3.6317 mL 7.2635 mL 18.1587 mL
10 mM 0.3632 mL 1.8159 mL 3.6317 mL 9.0794 mL
15 mM 0.2421 mL 1.2106 mL 2.4212 mL 6.0529 mL
20 mM 0.1816 mL 0.9079 mL 1.8159 mL 4.5397 mL
25 mM 0.1453 mL 0.7263 mL 1.4527 mL 3.6317 mL
30 mM 0.1211 mL 0.6053 mL 1.2106 mL 3.0265 mL
40 mM 0.0908 mL 0.4540 mL 0.9079 mL 2.2698 mL
50 mM 0.0726 mL 0.3632 mL 0.7263 mL 1.8159 mL
60 mM 0.0605 mL 0.3026 mL 0.6053 mL 1.5132 mL
80 mM 0.0454 mL 0.2270 mL 0.4540 mL 1.1349 mL
100 mM 0.0363 mL 0.1816 mL 0.3632 mL 0.9079 mL
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Physostigmine Related Classifications

  • 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.

Keywords:

Physostigmine57-47-6EserineCholinesterase (ChE)blood-brainbarrierAlzheimer'santidoteInhibitorinhibitorinhibit

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