| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| 10g |
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Purity: ≥98%
Ibuprofen piconol (U75630), the pyridyl ester of ibuprofen, is a potent non-steroidal, anti-inflammatory (NSAID) drug marketed in Japan for the topical relief of primary thermal burns and sunburns.
| ln Vitro |
Ibuprofen pyridinol is a liquid that exhibits no surface activity and partitions strongly into the oil phase. It is somewhat hygroscopic and chemically stable. It is miscible with less polar organic compounds, except silicone oils, and has extremely limited solubility in water (16.5 ppm), moderate solubility in glycerol (16.4 mg/mL), and both [1]. The hydrolysis half-life (concentration range: 50 to 200 μg/mL) remained unchanged when the starting concentration of ibuprofen pyridinol was changed. The hydrolysis half-life can change when anticoagulants are used. The half-lives of plasma (t1/2=2.5 hours) and citrate (t1/2=8.0 hours), heparin (t1/2 = 15.5 hours), and EDTA (t1/2 = 161.8 hours) vary depending on whether anticoagulant is present or not. Red blood cells absorb very little ibuprofen pyridinol, ranging from 0.4% to 4.1% of the amounts employed in research [2].
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| ln Vivo |
Only ibuprofen and its metabolites were found in plasma and urine after ibuprofen piconol was applied topically. Pyridol appears to be rapidly converted by the body to ibuprofen [2].
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| References |
[1]. Pesheck CV, et al. Preformulation characterization of topical Ibuprofen Piconol. Drug Development and Industrial Pharmacy Vol. 19 , Iss. 15,1993
[2]. Christensen JM, et al. Ibuprofen piconol hydrolysis in vitro in plasma, whole blood, and serum using different anticoagulants. J Pharm Sci. 1991 Jan;80(1):29-31. |
| Additional Infomation |
Ibuprofen piconol is an organic molecular entity.
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| Molecular Formula |
C19H23NO2
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|---|---|
| Molecular Weight |
297.3914
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| Exact Mass |
297.172
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| CAS # |
64622-45-3
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| PubChem CID |
3673
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.3
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
22
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| Complexity |
334
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ACEWLPOYLGNNHV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H23NO2/c1-14(2)12-16-7-9-17(10-8-16)15(3)19(21)22-13-18-6-4-5-11-20-18/h4-11,14-15H,12-13H2,1-3H3
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| Chemical Name |
2-Pyridylmethyl 2-(4-isobutylphenyl)propionate
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| Synonyms |
U-75630; U 75630; U75630; Ibuprofen piconol
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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 |
| 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 : ≥ 50 mg/mL (~168.13 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.41 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 (8.41 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 (8.41 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 | 3.3626 mL | 16.8129 mL | 33.6259 mL | |
| 5 mM | 0.6725 mL | 3.3626 mL | 6.7252 mL | |
| 10 mM | 0.3363 mL | 1.6813 mL | 3.3626 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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