| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Benoxinate targets voltage-gated sodium channels on the neuronal cell membrane. By binding to and blocking these channels, it prevents the propagation of action potentials. This inhibits the generation and conduction of nerve impulses, leading to a reversible loss of sensation in the area of application. Its action is local and does not affect the central nervous system when used topically.
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| ln Vitro |
In vitro, benoxinate blocks sodium channels in isolated nerve preparations. This can be demonstrated using electrophysiological techniques, such as patch-clamp, on neurons. It reduces the amplitude of compound action potentials in isolated nerves. Its potency as a sodium channel blocker is assessed by measuring the concentration required to reduce the action potential amplitude by 50%.
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| ln Vivo |
Rats treated with subcutaneous injection of benoxinate hydrochloride (27.6, 51.7, 103.5, 413.9 μg) exhibit a dose-dependent blocking effect on acupuncture [1]. 100% sensory/nociceptive blockage is produced by oxbuvacaine hydrochloride (27.6 μg) [1].
In vivo, benoxinate produces rapid anesthesia when applied topically to the eye. It penetrates the corneal epithelium and binds to sodium channels in the nerve endings, providing anesthesia within 30 seconds to 1 minute. The effect lasts for approximately 10-20 minutes, which is sufficient for short ophthalmic procedures. It does not cause mydriasis or cycloplegia, making it suitable for tonometry. |
| Enzyme Assay |
The in vitro receptor binding assay for benoxinate involves measuring its affinity for the voltage-gated sodium channel. This is typically done using a radioligand binding assay with [³H]-batrachotoxin or [³H]-saxitoxin, which bind to specific sites on the sodium channel. Competition binding experiments are performed to determine the Ki of benoxinate at the sodium channel.
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| Cell Assay |
In vitro cellular assays for benoxinate are performed on cultured neurons or on cells expressing voltage-gated sodium channels. The functional block of sodium channels is measured using electrophysiological techniques (patch-clamp). The reduction in sodium current (INa) upon application of benoxinate is quantified to determine its potency (IC50) and voltage-dependence of block.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (203-253 g) [1]
Doses: 27.6, 51.7, 103.5, 413.9 μg Route of Administration: SC Experimental Results: Provides dose-dependent blockade of acupuncture. In vivo animal experiments for benoxinate are typically conducted in rabbits or other laboratory animals. The compound is applied topically to the eye, and the corneal anesthetic effect is assessed by measuring the corneal touch threshold or the blink reflex. The onset of action and duration of anesthesia are recorded to evaluate its efficacy and duration of action. |
| ADME/Pharmacokinetics |
Benoxinate is a local anesthetic that is rapidly absorbed through the corneal epithelium. It is metabolized by plasma esterases in the blood and in the eye. The metabolites are excreted in the urine. The systemic absorption of benoxinate is minimal when used topically, so its systemic pharmacokinetics are not a significant concern. Its duration of action is short, typically 10-20 minutes.
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| Toxicity/Toxicokinetics |
Benoxinate is generally well-tolerated when used as a topical ophthalmic anesthetic. Common side effects are local and include transient stinging, burning, and redness of the eye. Prolonged or frequent use can lead to corneal epithelial damage and delayed wound healing. Systemic toxicity is rare due to minimal absorption, but can occur if large amounts are absorbed or injected accidentally.
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| References |
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| Additional Infomation |
Oxybuprocaine is a benzoic acid ester composed of 4-amino-3-butoxybenzoic acid and 2-(diethylamino)ethanol forming an ester bond; it is an ester-type local anesthetic (ester "caine"), particularly used in ophthalmology and otolaryngology. It has dual effects as a local anesthetic, surface anesthetic, and drug allergen. It is a benzoic acid ester, tertiary amine compound, substituted aniline, and amino acid ester. Its function is related to 2-diethylaminoethanol. Oxybuprocaine (also known as phenoxyamine) is a local anesthetic, particularly used in ophthalmology and otolaryngology. Oxybuprocaine binds to sodium ion channels, reversibly stabilizing neuronal membranes and thus reducing their permeability to sodium ions. See also: phenoxyamine hydrochloride (note moved to).
Drug Indications Used for temporary anesthesia of the anterior surface of the eyeball for measuring intraocular pressure or removing foreign bodies. Mechanism of Action Oxybuprocaine binds to sodium ion channels, reversibly stabilizing the neuronal membrane and reducing its permeability to sodium ions. Neuronal membrane depolarization is inhibited, thereby blocking the generation and conduction of nerve impulses. Pharmacodynamics Oxybuprocaine is a local anesthetic. Its irritant properties may be lower than tetracaine, and its onset and duration of action are similar. Benoxinate hydrochloride is marketed under the brand name Novesine. It is a standard anesthetic in ophthalmology, used for a variety of short diagnostic and minor surgical procedures. It is available as a 0.4% ophthalmic solution. It is a prescription drug and should only be used under the supervision of an ophthalmologist. It is one of the most commonly used topical anesthetics in eye care. |
| Molecular Formula |
C17H29CLN2O3
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|---|---|
| Molecular Weight |
344.8768
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| Exact Mass |
344.186
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| CAS # |
5987-82-6
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| Related CAS # |
Oxybuprocaine;99-43-4
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| PubChem CID |
4633
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| Appearance |
White to off-white solid powder
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| Boiling Point |
446.9ºC at 760 mmHg
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| Melting Point |
158 - 162ºC
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| Flash Point |
224.1ºC
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| LogP |
4.329
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
22
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| Complexity |
308
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CMHHMUWAYWTMGS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H28N2O3/c1-4-7-11-21-16-13-14(8-9-15(16)18)17(20)22-12-10-19(5-2)6-3/h8-9,13H,4-7,10-12,18H2,1-3H3
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| Chemical Name |
2-(diethylamino)ethyl 4-amino-3-butoxybenzoate
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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 : ≥ 100 mg/mL (~289.96 mM)
DMSO : ~100 mg/mL (~289.96 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.25 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 25.0 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: ≥ 2.5 mg/mL (7.25 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 25.0 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: ≥ 2.5 mg/mL (7.25 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 | 2.8996 mL | 14.4978 mL | 28.9956 mL | |
| 5 mM | 0.5799 mL | 2.8996 mL | 5.7991 mL | |
| 10 mM | 0.2900 mL | 1.4498 mL | 2.8996 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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