| Size | Price | Stock | Qty |
|---|---|---|---|
| 5g |
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| Other Sizes |
| Targets |
Benorilate's mechanism of action is derived from its two active metabolites: salicylic acid and paracetamol. Salicylic acid acts as a non-selective COX inhibitor, reducing prostaglandin synthesis to produce anti-inflammatory, analgesic, and antipyretic effects. Paracetamol is a centrally acting analgesic and antipyretic. Its mechanism is thought to involve the inhibition of COX-2 in the brain and the activation of descending serotonergic pain pathways.
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| ln Vitro |
Benorylate (Salipran) is an esterified aspirin product that has been shown to have antirheumatic characteristics comparable to aspirin [1]. Benorylate (Salipran) significantly reduces the liver's conversion of lactate to glucose, which is a key component of glucose homeostasis. Benorylate (Salipran) also reduces the rate of ammonia urea production, another crucial liver function [2].
In vitro, benorilate itself has minimal activity until it is hydrolyzed to its active components. The individual metabolites, salicylic acid and paracetamol, exhibit their respective pharmacological activities. Salicylic acid inhibits COX enzymes, while paracetamol acts as a weak COX inhibitor in the presence of peroxides, which are abundant in inflammatory tissues. |
| ln Vivo |
Salipran's good stomach tolerance is likely due to its absorption as an intact molecule [3]. In both human tissues and experimental animals, benorylate (Salipran) has the ability to suppress PG production [4].
In vivo, benorilate is used as an analgesic and antipyretic for the relief of mild to moderate pain and fever. It has been used in the treatment of conditions such as osteoarthritis, rheumatoid arthritis, and other musculoskeletal disorders. Its combined action provides both peripheral (salicylate) and central (paracetamol) analgesia, offering a broad spectrum of pain relief. |
| Enzyme Assay |
The in vitro enzyme inhibition assay for benorilate involves measuring the activity of the metabolites. Salicylic acid's inhibition of COX-1 and COX-2 is assessed using standard enzyme assays. Paracetamol's activity is more complex and is often measured by its ability to inhibit prostaglandin synthesis in a cell-based system or by its effect on pain pathways in vivo.
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| Cell Assay |
In vitro cellular assays for benorilate are typically performed using the individual metabolites. For example, the anti-inflammatory effect of salicylic acid can be measured by its ability to inhibit the production of PGE2 in LPS-stimulated macrophages. The analgesic effect of paracetamol is more difficult to assess in vitro and is usually studied in animal models.
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| Animal Protocol |
In vivo animal experiments for benorilate were conducted using standard models of pain and inflammation. The carrageenan-induced paw edema model in rats was used to assess its anti-inflammatory effect. The analgesic effect was evaluated using the tail-flick test or the hot-plate test in mice. The antipyretic effect was assessed in yeast-induced pyrexia models in rats.
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| ADME/Pharmacokinetics |
After oral administration, benorilate is rapidly and almost completely absorbed. It undergoes extensive first-pass metabolism in the liver, where it is hydrolyzed to salicylic acid and paracetamol. The pharmacokinetics of benorilate are essentially the sum of the pharmacokinetics of its two metabolites. Salicylic acid has a half-life of 2-4 hours at low doses, while paracetamol has a half-life of 1-3 hours.
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| Toxicity/Toxicokinetics |
Benorilate shares the side effect profile of both salicylates and paracetamol. Common side effects include gastrointestinal irritation, nausea, and dyspepsia, similar to aspirin. It can also cause hepatotoxicity in overdose, similar to paracetamol. Rarely, it can cause allergic reactions and tinnitus. It is contraindicated in patients with aspirin allergy, liver disease, or severe renal impairment.
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| References | |
| Additional Infomation |
Benorilate is a carbonyl compound.
Benorilate was developed and marketed under the brand name Benoral. It was used as an alternative to aspirin and paracetamol, particularly in patients who were intolerant to aspirin due to gastrointestinal side effects. However, its use has declined with the availability of other NSAIDs and the widespread use of paracetamol. It is not a commonly used drug today. |
| Molecular Formula |
C17H15NO5
|
|---|---|
| Molecular Weight |
313.3047
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| Exact Mass |
313.095
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| CAS # |
5003-48-5
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| PubChem CID |
21102
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
511.5±60.0 °C at 760 mmHg
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| Melting Point |
177-181ºC
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| Flash Point |
263.1±32.9 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.566
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| LogP |
2.22
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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 |
6
|
| Heavy Atom Count |
23
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| Complexity |
442
|
| Defined Atom Stereocenter Count |
0
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| InChi Key |
FEJKLNWAOXSSNR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H15NO5/c1-11(19)18-13-7-9-14(10-8-13)23-17(21)15-5-3-4-6-16(15)22-12(2)20/h3-10H,1-2H3,(H,18,19)
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| Chemical Name |
(4-acetamidophenyl) 2-acetyloxybenzoate
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~125 mg/mL (~398.98 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.64 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 (6.64 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 (6.64 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 | 3.1918 mL | 15.9591 mL | 31.9183 mL | |
| 5 mM | 0.6384 mL | 3.1918 mL | 6.3837 mL | |
| 10 mM | 0.3192 mL | 1.5959 mL | 3.1918 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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