| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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Esflurbiprofen (BTS-24332; TT 063; BTS24332; TT063; SFPP; BTS 24332; TT-063; Trade name: Loqoa), the S-enantiomrer or S-isomer of Flurbiprofen, is a potent cyclooxygenase (COX) inhibitor and a nonsteroidal anti-inflammatory drugs (NSAIDs) with antipyretic and analgesic activity.
| ln Vitro |
(S)-Flurbiprofen (10–7 M) completely transcribes the dye's basal and induced PGE2 release [2].
|
|---|---|
| ADME/Pharmacokinetics |
Metabolism / Metabolites
(s)-flurbiprofen has known human metabolites that include 4-hydroxy-S-flurbiprofen. |
| References |
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| Additional Infomation |
(S)-flurbiprofen is a flurbiprofen. It is an enantiomer of a (R)-flurbiprofen.
Esflurbiprofen is under investigation in clinical trial NCT03434197 (Safety and Efficacy of SFPP in Knee Osteoarthritis). |
| Molecular Formula |
C15H13FO2
|
|---|---|
| Molecular Weight |
244.2654
|
| Exact Mass |
244.089
|
| CAS # |
51543-39-6
|
| PubChem CID |
72099
|
| Appearance |
White to off-white solid powder
|
| Density |
1.2±0.1 g/cm3
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| Boiling Point |
376.2±30.0 °C at 760 mmHg
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| Melting Point |
109-110ºC(lit.)
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| Flash Point |
181.3±24.6 °C
|
| Vapour Pressure |
0.0±0.9 mmHg at 25°C
|
| Index of Refraction |
1.568
|
| LogP |
4.11
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
18
|
| Complexity |
286
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C[C@@H](C1=CC(=C(C=C1)C2=CC=CC=C2)F)C(=O)O
|
| InChi Key |
SYTBZMRGLBWNTM-JTQLQIEISA-N
|
| InChi Code |
InChI=1S/C15H13FO2/c1-10(15(17)18)12-7-8-13(14(16)9-12)11-5-3-2-4-6-11/h2-10H,1H3,(H,17,18)/t10-/m0/s1
|
| Chemical Name |
(2S)-2-(3-fluoro-4-phenylphenyl)propanoic acid
|
| Synonyms |
BTS-24332; TT 063; BTS24332; TT063; SFPP; BTS 24332; TT-063; Trade name: Loqoa
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~409.40 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.23 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0938 mL | 20.4692 mL | 40.9383 mL | |
| 5 mM | 0.8188 mL | 4.0938 mL | 8.1877 mL | |
| 10 mM | 0.4094 mL | 2.0469 mL | 4.0938 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04908748 | Completed | Drug: Esflurbiprofen Hydrogel Patch | Bruises Contusions Soft Tissue Injuries Sprains Strains |
Teikoku Seiyaku Co., Ltd. | 2021-05-20 | Phase 2 |
| NCT02729207 | Terminated | Drug: Esflurbiprofen Hydrogel Patch | Ankle Sprain | Teikoku Seiyaku Co., Ltd. | 2016-07 | Phase 2 |
| NCT03434197 | Completed | Drug: Esflurbiprofen Drug: Diclofenac diethylamine |
Osteoarthritis Knee Pain | Taisho Pharmaceutical Co., Ltd. | 2018-02-05 | Phase 3 |
| NCT04505787 | Completed | Drug: Esflurbiprofen hydrogel patch 165 mg (EFHP) Drug: Froben 100 mg comprimidos revestidos |
Comparative Bioavailability | SocraTec R&D GmbH | 2020-07-24 | Phase 1 |
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