Physostigmine
Based on 2 publication(s) in Google Scholar
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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- Purity: 99.89%
- CAS No.: 57-47-6
- 화학식: C15H21N3O2
- 분자량:275.35
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Physostigmine
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.16 μM
Compound: Eserine
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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
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10.1039/C1MD00221J |
| Sf21 | IC50 |
>1000 μM
Compound: Physostigmine
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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
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[PMID: 21965623] |
| Sf21 | IC50 |
>1000 μM
Compound: Physostigmine
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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
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[PMID: 21965623] |
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.
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Animal Model:Heterozygous transgenic mice (Tg(+) mice)[2]
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Dosage:0.03, 0.1, and 0.3 mg/kg
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Administration:SC; daily for 6 weeks
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Result:Tended to normalize the contextual memory deficit in Tg(+) animals so that they became more similar to Tg(-) animals.
Chemical Information
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CAS No. 57-47-6
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Appearance Solid
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분자량 275.35
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화학식 C15H21N3O2
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Color Light yellow to brown
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SMILES
CN1[C@](N(C)CC2)([H])[C@]2(C)C3=C1C=CC(OC(NC)=O)=C3
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Synonyms
Eserine
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Structure Classification
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Initial Source
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (277 KB)
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SDS (482 KB)
- English - EN (482 KB)
- Français - FR (482 KB)
- Deutsch - DE (482 KB)
- Norwegian - NO (482 KB)
- Español - ES (482 KB)
- Swedish - SV (482 KB)
- Italian - IT (482 KB)
- Korean - KR (482 KB)
- Portuguese - PT (482 KB)
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Handling Instructions (2659 KB)
References
[1]. Haase U, et al. Pharmakotherapie--physostigmin post OP [Pharmacotherapy--physostigmine administered post-operatively]. Anasthesiol Intensivmed Notfallmed Schmerzther. 2007;42(3):188‐189. [Content Brief]
[2]. Dong H, et al, Bertchume A, Vallera D, Csernansky JG. Acetylcholinesterase inhibitors ameliorate behavioral deficits in the Tg2576 mouse model of Alzheimer's disease. Psychopharmacology (Berl). 2005;181(1):145‐152. [Content Brief]
[3]. Frascogna N. Physostigmine: is there a role for this antidote in pediatric poisonings? Curr Opin Pediatr. 2007;19(2):201‐205. [Content Brief]
[4]. Jonathan D Kenny, et al. Physostigmine and Methylphenidate Induce Distinct Arousal States During Isoflurane General Anesthesia in Rats. Anesth Analg. 2016 Nov;123(5):1210-1219. [Content Brief]
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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