| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
Physostigmine salicylate targets acetylcholinesterase (AChE). It is a reversible cholinesterase inhibitor. The salicylate salt form improves the solubility of the compound for medical applications. It crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Its IC50 for AChE inhibition is comparable to that of physostigmine (0.67 nM).
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| ln Vitro |
Physostigmine salicylate demonstrates potent AChE inhibition in vitro with an IC50 comparable to physostigmine (0.67 nM). As a reversible cholinesterase inhibitor, it prevents the breakdown of acetylcholine at synapses, leading to increased cholinergic neurotransmission. Its activity is assessed in enzymatic assays using purified AChE or tissue homogenates.
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| ln Vivo |
To enhance threat memory and cue memory impairments in Tg(+) mice, physostigmine salicylate (also known as Eserine salicylate; 0.03-0.3 mg/kg; sc; once daily for 6 weeks) is administered [2].
Physostigmine salicylate is used clinically as a reversible cholinesterase inhibitor. It is used primarily in the treatment of glaucoma, Alzheimer's disease, and anticholinergic toxicity. It crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. It is available as bulk pharmaceuticals for parasympathomimetic, cholinergic, ophthalmic, and anti-Alzheimer applications. |
| Enzyme Assay |
Acetylcholinesterase inhibition assays are performed using recombinant or purified AChE enzyme. The enzyme is incubated with the substrate acetylthiocholine in the presence of varying concentrations of Physostigmine salicylate. The reaction product (thiocholine) is detected using Ellman's reagent (DTNB), which produces a yellow color measured spectrophotometrically at 412 nm. Inhibition is calculated as a percentage of control activity. IC50 values are determined by non-linear regression analysis. Each concentration is tested in duplicate or triplicate.
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| Cell Assay |
Cellular AChE inhibition is evaluated in neuronal cell lines (e.g., SH-SY5Y) or primary neuronal cultures. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with Physostigmine salicylate at various concentrations (0.001-10 µM). AChE activity in cell lysates is measured using the Ellman's assay. Acetylcholine levels can be quantified by HPLC or ELISA. Cell viability is assessed using MTT or LDH assays. Each experiment includes known AChE inhibitors as positive controls and vehicle controls.
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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 studies are conducted in animal models of glaucoma, Alzheimer's disease, or anticholinergic toxicity. Physostigmine salicylate is administered intravenously, intraperitoneally, or topically (ocular) at doses determined by preclinical studies. For glaucoma studies, intraocular pressure is measured. For anticholinergic toxicity studies, reversal of toxicity symptoms is assessed. Sample sizes typically range from 6-10 animals per group. Clinical studies have been conducted for these indications. |
| ADME/Pharmacokinetics |
Physostigmine salicylate has a molecular weight of 413.47 g/mol and a molecular formula of C22H27N3O5. CAS Registry Number: 57-64-7. It is classified as super toxic in some references. The salicylate form improves the solubility of physostigmine, making it easier to administer in medical applications. Storage: typically at room temperature, protected from light and moisture.
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| Toxicity/Toxicokinetics |
Physostigmine salicylate is generally well-tolerated at therapeutic doses. Common adverse effects may include nausea, vomiting, diarrhea, sweating, and bradycardia due to increased cholinergic activity. Overdose can cause cholinergic crisis. It is contraindicated in patients with asthma, cardiovascular disease, and gastrointestinal obstruction. Standard toxicology studies have demonstrated an acceptable safety profile for its approved uses.
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| References |
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| Additional Infomation |
Crystal form, turns red upon heating or exposure to light. (EPA, 1998)
Physostigmine salicylate is a nitrogen-containing heterocyclic salicylate, belonging to the salicylate class of compounds. It contains physostigmine. See also: Physostigmine (with active moiety). Physostigmine salicylate is also known as Eserine salicylate. It is the salicylate salt of physostigmine (eserine). It is a reversible acetylcholinesterase inhibitor used in glaucoma, Alzheimer's disease, and anticholinergic toxicity. It crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. It is approved for clinical use in many countries. |
| Molecular Formula |
C22H27N3O5
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|---|---|
| Molecular Weight |
413.46688
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| Exact Mass |
413.195
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| CAS # |
57-64-7
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| Related CAS # |
Physostigmine hemisulfate;64-47-1;Physostigmine;57-47-6
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| PubChem CID |
657348
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| Appearance |
White to yellow solid powder
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| Boiling Point |
393.5ºC at 760 mmHg
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| Melting Point |
181-183 °C
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| Flash Point |
191.8ºC
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| LogP |
3.258
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
535
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C[C@@]12CCN([C@@H]1N(C3=C2C=C(C=C3)OC(=O)NC)C)C.C1=CC=C(C(=C1)C(=O)O)O
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| InChi Key |
HZOTZTANVBDFOF-PBCQUBLHSA-N
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| InChi Code |
InChI=1S/C15H21N3O2.C7H6O3/c1-15-7-8-17(3)13(15)18(4)12-6-5-10(9-11(12)15)20-14(19)16-28-6-4-2-1-3-5(6)7(9)10/h5-6,9,13H,7-8H2,1-4H3,(H,16,19)1-4,8H,(H,9,10)/t13-,15+/m1./s1
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| Chemical Name |
Benzoic acid, 2-hydroxy-, compd. with
(3aS,8aR)-1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethylpyrrolo(2,3-b)indol-5-yl
methylcarbamate (1
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| Synonyms |
Physostigmine salicylate Antilirium AR-44 CCRIS
3405 EINECS 200-343-8 Isopto Eserine Physostigmine monosalicylate.
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
DMSO : ~125 mg/mL (~302.32 mM)
H2O : ~33.33 mg/mL (~80.61 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5 mg/mL (12.09 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4186 mL | 12.0928 mL | 24.1856 mL | |
| 5 mM | 0.4837 mL | 2.4186 mL | 4.8371 mL | |
| 10 mM | 0.2419 mL | 1.2093 mL | 2.4186 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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