| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
Physostigmine targets cholinesterase enzymes, including acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). By inhibiting these enzymes, it prevents the breakdown of the neurotransmitter acetylcholine, leading to an accumulation of acetylcholine at cholinergic synapses. This enhances cholinergic transmission.
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| ln Vitro |
In vitro, physostigmine hemisulfate is a potent and reversible inhibitor of cholinesterase. Its activity is typically assessed by measuring its ability to inhibit the hydrolysis of acetylthiocholine by AChE. Its potency and reversible nature make it a valuable tool for studying cholinergic systems.
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| ln Vivo |
Eserine hemisulfate (Eserine hemisulfate; 0.03-0.3 mg/kg; subcutaneous injection; once daily for 6 weeks) can enhance contextual memory and cued memory deficits in Tg(+) mice [2]. Physostigmine hemisulfate (IV; 0.1, 0.2 mg/kg) delayed awakening from isoflurane anesthesia in male Sprague-Dawley rats at dosages ≥0.2 mg/kg [4].
In vivo, physostigmine is a well-known cholinergic agent. It can cross the blood-brain barrier and has been used clinically (as physostigmine salicylate) to reverse the effects of anticholinergic drugs and to treat conditions like glaucoma. The hemisulfate salt is a research analog. |
| Enzyme Assay |
The in vitro enzyme assay for physostigmine hemisulfate is a standard cholinesterase inhibition assay. It uses the Ellman's method, where the enzyme (AChE) hydrolyzes acetylthiocholine to thiocholine, which reacts with DTNB to produce a yellow color. The compound's ability to inhibit this reaction is measured spectrophotometrically.
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| Cell Assay |
In vitro cellular studies are not typical for physostigmine hemisulfate, as its target is an enzyme, not a cellular receptor. Its effects are studied in tissue preparations or in cell-free enzyme assays. However, it can be used in cell cultures to study the effects of enhanced cholinergic signaling.
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| Animal Protocol |
Animal/Disease Models: Heterozygous transgenic mice (Tg(+) mice) [2]
Doses: 0.03, 0.1 and 0.3 mg/kg Route of Administration: SC; one time/day for 6 weeks Experimental Results: Tg(+) Animal Situation Memory deficits normalized, causing them to become more similar to Tg(-) animals. In vivo animal experiments are performed in models of cholinergic function. Physostigmine is administered to animals (e.g., rodents) to study its effects on behavior, cognition, and physiological parameters. These studies help to understand the role of acetylcholine in various brain functions and to evaluate potential therapeutic agents. |
| ADME/Pharmacokinetics |
Physostigmine hemisulfate has a molecular formula of C15H21N3O2·1/2H2SO4 and a molecular weight of 324.39 g/mol. It is soluble in water (32 mg/mL). For research, it is typically stored at 2-8°C in a refrigerator under an inert atmosphere as it is hygroscopic. Its purity is often ≥98%.
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| Toxicity/Toxicokinetics |
As a potent cholinesterase inhibitor, physostigmine hemisulfate is highly toxic. It is not intended for human use as a research chemical. It should be handled with extreme care, using appropriate safety precautions to avoid exposure. Its toxicity is related to its mechanism of action: overstimulation of cholinergic receptors.
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| References |
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| Additional Infomation |
Physostigmine hemisulfate is a research analog of the cholinesterase inhibitor physostigmine. It is used as a pharmacological tool to study cholinergic neurotransmission and as a standard in enzyme inhibition assays. It is a controlled substance in many jurisdictions due to its toxicity and is available for research purposes only.
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| Molecular Formula |
(C15H21N3O2)2.H2SO4
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|---|---|
| Molecular Weight |
373.42462
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| Exact Mass |
648.294
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| CAS # |
64-47-1
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| Related CAS # |
Physostigmine salicylate;57-64-7;Physostigmine;57-47-6
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| PubChem CID |
6419928
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| Appearance |
White to off-white solid powder
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| Boiling Point |
557.5ºC at 760 mmHg
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| Flash Point |
291ºC
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| LogP |
4.763
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
45
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| Complexity |
484
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C[C@@]12CCN([C@@H]1N(C3=C2C=C(C=C3)OC(=O)NC)C)C.C[C@@]12CCN([C@@H]1N(C3=C2C=C(C=C3)OC(=O)NC)C)C.OS(=O)(=O)O
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| InChi Key |
YYBNDIVPHIWTPK-KYJQVDHRSA-N
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| InChi Code |
InChI=1S/2C15H21N3O2.H2O4S/c2*1-15-7-8-17(3)13(15)18(4)12-6-5-10(9-11(12)15)20-14(19)16-2;1-5(2,3)4/h2*5-6,9,13H,7-8H2,1-4H3,(H,16,19);(H2,1,2,3,4)/t2*13-,15+;/m11./s1
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| Chemical Name |
[(3aR,8bS)-3,4,8b-trimethyl-2,3a-dihydro-1H-pyrrolo[2,3-b]indol-7-yl] N-methylcarbamate;sulfuric acid
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| Synonyms |
AR44 CCRIS3405AR-44 CCRIS-3405AR 44 CCRIS 3405Eserine Antilirium Physostol Esromiotin Ezerin
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~50 mg/mL (~154.14 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6779 mL | 13.3897 mL | 26.7795 mL | |
| 5 mM | 0.5356 mL | 2.6779 mL | 5.3559 mL | |
| 10 mM | 0.2678 mL | 1.3390 mL | 2.6779 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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