| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
| Targets |
Edrophonium targets acetylcholinesterase (AChE), the enzyme responsible for hydrolyzing acetylcholine in the synaptic cleft. As a reversible, competitive inhibitor, it binds to the active site of AChE, preventing the breakdown of acetylcholine. This increases the concentration of acetylcholine at the neuromuscular junction and other cholinergic synapses, enhancing cholinergic neurotransmission.
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|---|---|
| ln Vitro |
In vitro, edrophonium inhibits acetylcholinesterase activity. Its potency has been characterized in enzymatic assays using purified AChE or tissue homogenates. The compound's rapid onset and short duration of action have been demonstrated. As a reversible inhibitor, its effects are dependent on the presence of the compound and can be overcome by high concentrations of substrate.
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| ln Vivo |
In vivo, edrophonium is used as a diagnostic agent for myasthenia gravis (Tensilon test). It is also used as an antidote for neuromuscular blockade caused by competitive neuromuscular blockers. Its rapid onset and short duration of action make it suitable for diagnostic applications. The compound increases muscle strength in patients with myasthenia gravis.
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| Enzyme Assay |
In vitro enzyme assays for edrophonium measure acetylcholinesterase inhibition. AChE enzyme (from electric eel or recombinant sources) is incubated with a chromogenic substrate (e.g., acetylthiocholine) in the presence of Ellman's reagent (DTNB). Various concentrations of edrophonium are added. Enzyme activity is measured spectrophotometrically by monitoring the formation of the yellow TNB anion. IC50 values are calculated.
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| Cell Assay |
Cellular assays for edrophonium are not typically performed, as it is a well-characterized AChE inhibitor. However, electrophysiological studies in neuromuscular preparations can assess the compound's effects on synaptic transmission. Muscle contractions are measured in response to nerve stimulation in the presence of various concentrations of edrophonium.
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| Animal Protocol |
In vivo animal studies for edrophonium utilize animal models of neuromuscular blockade. The compound is administered intravenously. Muscle strength is assessed by measuring grip strength or by electromyography. Reversal of neuromuscular blockade is evaluated. Efficacy is compared to vehicle and reference AChE inhibitors (e.g., neostigmine).
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| ADME/Pharmacokinetics |
Edrophonium chloride has molecular weight of 201.69 g/mol and molecular formula C10H16ClNO. It is a crystalline solid. It is soluble in water (>10%) and moderately soluble in alcohol. Melting point is 151-152°C (dec.). It is typically stored at room temperature. Solutions are stable. Pharmacokinetic properties include rapid onset and short duration of action.
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| Toxicity/Toxicokinetics |
Edrophonium chloride has a well-established safety profile but can cause adverse effects. Common adverse effects include bradycardia, hypotension, nausea, vomiting, and excessive salivation, which are due to enhanced cholinergic transmission. Overdose can cause cholinergic crisis (muscle weakness, respiratory depression). Atropine is used as an antidote for muscarinic effects.
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| Additional Infomation |
Edrophonium chloride is the chloride form of eosinamide chloride. It is a reversible cholinesterase inhibitor with a rapid onset of action (30-60 seconds after injection) but a short duration of action (5-15 minutes). In the diagnosis of myasthenia gravis, it can be used both for diagnosis and to differentiate between insufficient or excessive treatment with other anticholinesterase drugs. It has also been used to reverse neuromuscular blocks during anesthesia and to treat tetrodotoxin poisoning. Tetrodotoxin is a neuromuscular blocking toxin found in pufferfish and other marine animals. It can be used as an EC 3.1.1.8 (cholinesterase) inhibitor, diagnostic agent, and antidote. It is a quaternary ammonium salt and chloride containing an eosinamide chloride group. Edrophonium chloride is the chloride form of eosinamide chloride, a short-acting, rapid-acting cholinesterase inhibitor with parasympathomimetic activity. Edrophonium chloride enhances the action of endogenous acetylcholine by inhibiting acetylcholinesterase, which hydrolyzes acetylcholine. When applied topically to the eye, this drug prolongs the stimulation of parasympathetic receptors at the neuromuscular junction of the longitudinal muscles of the ciliary body. Contraction of the longitudinal muscles pulls on the scleral spurs, opening the trabecular meshwork, thereby increasing aqueous humor outflow and lowering intraocular pressure. It is a rapidly acting, short-acting cholinesterase inhibitor used to treat arrhythmias and diagnose myasthenia gravis. It has also been used as an antidote for curare. See also: atropine sulfate; ephemeral chloride (component).
Edrophonium Chloride is a readily reversible acetylcholinesterase inhibitor. It has a rapid onset and short duration of action. It is used as a diagnostic agent for myasthenia gravis and as an antidote for neuromuscular blockade. It is a clinically approved drug. |
| Molecular Formula |
C10H16CLNO
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|---|---|
| Molecular Weight |
201.69
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| Exact Mass |
201.092
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| CAS # |
116-38-1
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| Related CAS # |
Edrophonium-d5 chloride
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| PubChem CID |
8307
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| Appearance |
White to light yellow solid powder
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| Density |
1.395 g/mL at 25 °C(lit.)
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| Boiling Point |
130 °C20 mm Hg(lit.)
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| Melting Point |
162-163°C
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| Flash Point |
>230 °F
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| Index of Refraction |
n20/D 1.486(lit.)
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
13
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| Complexity |
145
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BXKDSDJJOVIHMX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H15NO.ClH/c1-4-11(2,3)9-6-5-7-10(12)8-9;/h5-8H,4H2,1-3H3;1H
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| Chemical Name |
ethyl-(3-hydroxyphenyl)-dimethylazanium;chloride
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| Synonyms |
Tensilon chloride; Tensilon; Edrophonium Chloride
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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 : ~62.5 mg/mL (~309.88 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.31 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 (10.31 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 (10.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.9581 mL | 24.7905 mL | 49.5810 mL | |
| 5 mM | 0.9916 mL | 4.9581 mL | 9.9162 mL | |
| 10 mM | 0.4958 mL | 2.4791 mL | 4.9581 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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