| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Kidneys: Primarily through renal hydrolysis. Metabolism/Metabolites: This drug is hydrolyzed by plasma esterases in both plasma and liver. |
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| Additional Infomation |
Prooxycaine is a benzoic acid ester. Prooxycaine is an ester-based local anesthetic with a rapid onset of action and a longer duration of action than procaine hydrochloride. It was withdrawn from the US market in 1996. Although no longer sold in the US, it was used in combination with procaine as an adjunct to dental anesthesia. When used in combination with procaine, it was the only dental local anesthetic available in cartridge form. Prooxycaine is a para-aminobenzoic acid ester with local anesthetic activity. Prooxycaine binds to and inhibits the activity of voltage-gated sodium channels, thereby inhibiting the ion flow required for nerve impulse initiation and conduction. This results in loss of sensation. An ester-based local anesthetic with a rapid onset of action and a longer duration of action than procaine hydrochloride. (Excerpt from Martindale Pharmacopoeia, 30th edition, p. 1017)
Drug Indications Prooxycaine is a local anesthetic. It has been used in dental surgery since the 1950s. It is often used in combination with procaine to accelerate onset and provide a longer-lasting anesthetic effect. Prooxycaine was developed for use when amide-based local anesthetics are contraindicated due to allergy or when multiple amide-based anesthetics are ineffective. Mechanism of Action Prooxycaine is a para-aminobenzoic acid ester with local anesthetic activity. Prooxycaine binds to voltage-gated sodium channels and blocks their permeability, thereby inhibiting the ion flow necessary for nerve impulse conduction. This leads to loss of sensation. One study showed that propyloxycaine hydrochloride increases the fluidity of cyclic lipids in the cellular lipid bilayer, with a stronger enhancing effect on the inner monolayer than the outer monolayer. This may further confirm its role in regulating nerve impulses. Pharmacodynamics Prooxycaine is a local anesthetic whose mechanism of action is to reduce nerve impulses, thereby alleviating pain during dental procedures. |
| Molecular Formula |
C16H26N2O3.HCL
|
|---|---|
| Molecular Weight |
330.85018
|
| Exact Mass |
330.171
|
| CAS # |
550-83-4
|
| PubChem CID |
6843
|
| Appearance |
White to light brown solid powder
|
| Boiling Point |
434.4ºC at 760mmHg
|
| Melting Point |
146-151
|
| Flash Point |
216.5ºC
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| LogP |
3.939
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
21
|
| Complexity |
295
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
CAJIGINSTLKQMM-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H26N2O3/c1-4-10-20-15-12-13(17)7-8-14(15)16(19)21-11-9-18(5-2)6-3/h7-8,12H,4-6,9-11,17H2,1-3H3
|
| Chemical Name |
2-(diethylamino)ethyl 4-amino-2-propoxybenzoate
|
| 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)
|
| Solubility (In Vitro) |
H2O : ~100 mg/mL (~302.25 mM)
DMSO : ~50 mg/mL (~151.13 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.29 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 (6.29 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 (6.29 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: ≥ 100 mg/mL (302.25 mM) (saturation unknown) in PBS (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 | 3.0225 mL | 15.1126 mL | 30.2252 mL | |
| 5 mM | 0.6045 mL | 3.0225 mL | 6.0450 mL | |
| 10 mM | 0.3023 mL | 1.5113 mL | 3.0225 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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