| Size | Price | |
|---|---|---|
| Other Sizes |
| ln Vitro |
(S)-(+)-ibuprofen treatment (HCT-15 and HCA-7 cells; 0-1000 µM; 8 days) decreased concentration-dependent cell survival in both cell lines to a comparable degree [2]. G0/G1 arrest and apoptosis are the outcomes of (S)-(+)-ibuprofen treatment (HCT-15 and HCA-7 cells; 0-1000 µM; 20-72 hours) [2]. (S)-(+)-ibuprofen treatment (HCT-15 and HCA-7 cells; 900 µM; 4-72 hours) resulted in an increase in the cell cycle inhibitory protein p27Kip-1 and a downregulation of cyclins A and B [2]. Platelet aggregation, thromboxane production, and COX activity are all inhibited by (S)-(+)-ibuprofen [1]. (S)-(+)-Ibuprofen, with an IC50 of 61.7 μM, prevents NF-κB from activating upon T cell stimulation [3].
|
|---|---|
| ln Vivo |
In nude mice models, treatment with (15 mg/kg/day; i.p.; five days per week; for four weeks) suppresses the formation of tumors in HCA-7 and HCT-15 xenografts [2].
|
| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: HCT-15 and HCA-7 Cell Tested Concentrations: 0 µM, 200 µM, 400 µM, 600 µM, 700 µM, 800 µM, 900 µM and 1000 µM Incubation Duration: 8 days Experimental Results: Two The concentration-dependent decrease in cell viability was similar among the cell lines. Cell cycle analysis[2] Cell Types: HCT-15 and HCA-7 Cell Tested Concentrations: 0 µM, 200 µM, 400 µM, 600 µM, 800 µM, 900 µM and 1000 µM Incubation Duration: 24 hrs (hours) (HCT-15) or 20 hrs (hours) (HCA-7) Experimental Results: Causes G0/G1 phase obstruction. Apoptosis analysis[2] Cell Types: HCT-15 and HCA-7 Cell Tested Concentrations: 0 µM, 200 µM, 400 µM, 600 µM, 800 µM, 900 µM and 1000 µM Incubation Duration: 72 hrs (hours) Experimental Results: Induction of apoptosis Death. Western Blot Analysis[2] Cell Types: HCT-15 and HCA-7 Cell Tested Concentrations: 900 µM Incubation Duration: 4 hrs (hours), 8 hrs (hours), 16 hrs (hours), 24 hrs (hours), 32 hrs (hours), 48 hrs (hours) and 72 hrs (hours) Experimental Results: Cyclin levels diminished D1 protein. |
| Animal Protocol |
Animal/Disease Models: NMRI (nu/nu) male mice (6-8 weeks old) injected with HCA-7 and HCT-15 cells [2]
Doses: 15 mg/kg/day Route of Administration: intraperitoneal (ip) injection; five days per week; continuous 4-week Experimental Results: Inhibition of tumor growth in mouse HCA-7 and HCT-15 xenografts. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Following oral administration of a tablet containing 300 mg dextroibuprofen, the time to peak plasma concentration is 2.25–5 hours. For more information, see [Ibuprofen]. It is primarily excreted via the kidneys. For more information, see [Ibuprofen]. For more information, see [Ibuprofen]. For more information, see [Ibuprofen]. For more information, see [Ibuprofen]. Metabolisms/Metabolites For more information, see [Ibuprofen]. Known metabolites of (S)-(+)-ibuprofen include 2-hydroxyibuprofen and 3-hydroxyibuprofen. Biological Half-Life The half-life of an oral 300 mg dextroibuprofen tablet is 2.2–4.7 hours. For more information, see [Ibuprofen]. |
| Toxicity/Toxicokinetics |
Protein Binding
For more information, please refer to [ibuprofen]. |
| References |
|
| Additional Infomation |
Dextrorotatory ibuprofen is a type of ibuprofen. It is a non-narcotic analgesic and a nonsteroidal anti-inflammatory drug (NSAID). It is the enantiomer of levorotatory ibuprofen. Dextrorotatory ibuprofen, or S(+)-ibuprofen, is a nonsteroidal anti-inflammatory drug (NSAID). It is the pharmacologically active enantiomer of racemic ibuprofen, and its physicochemical properties differ from those of racemic ibuprofen. Due to the higher concentration of the active S enantiomer, dextrorotatory ibuprofen is considered to have higher pharmacological activity, better tolerability, and better safety than ibuprofen. Compared to racemic ibuprofen, dextrorotatory ibuprofen dissolves more slowly in simulated gastric and intestinal fluids and has higher oral bioavailability. For information on metabolism, enzymes, carriers, and transport proteins, please refer to [Ibuprofen]. See also: Ibuprofen (note moved to).
Drug Indications For more information, please refer to [Ibuprofen]. Mechanism of Action Similar to common nonsteroidal anti-inflammatory drugs (NSAIDs), dextro-ibuprofen is the active enantiomer of ibuprofen. It inhibits prostaglandin synthesis in inflammatory cells by inhibiting the COX-2 isoenzyme of arachidonic acid cyclooxygenase (COX). For more information, please refer to [ibuprofen]. Pharmacodynamics For more information, please refer to [ibuprofen]. |
| Exact Mass |
206.13
|
|---|---|
| CAS # |
51146-56-6
|
| Related CAS # |
Ibuprofen;15687-27-1;(S)-(+)-Ibuprofen-d3;1329643-44-8;(R)-(-)-Ibuprofen;51146-57-7;Ibuprofen sodium;31121-93-4;Ibuprofen-d3;121662-14-4
|
| PubChem CID |
39912
|
| Appearance |
White to off-white solid powder
|
| Density |
1.0±0.1 g/cm3
|
| Boiling Point |
319.6±11.0 °C at 760 mmHg
|
| Melting Point |
49-53ºC
|
| Flash Point |
216.7±14.4 °C
|
| Vapour Pressure |
0.0±0.7 mmHg at 25°C
|
| Index of Refraction |
1.519
|
| LogP |
3.72
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
15
|
| Complexity |
203
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
OC([C@H](C1=CC=C(CC(C)C)C=C1)C)=O
|
| InChi Key |
HEFNNWSXXWATRW-JTQLQIEISA-N
|
| InChi Code |
InChI=1S/C13H18O2/c1-9(2)8-11-4-6-12(7-5-11)10(3)13(14)15/h4-7,9-10H,8H2,1-3H3,(H,14,15)/t10-/m0/s1
|
| Chemical Name |
(2S)-2-[4-(2-methylpropyl)phenyl]propanoic acid
|
| Synonyms |
L-669,455, MK 233 Dexibuprofen (free acid) MK-233Dexibuprofen Doctrin L 669455
|
| 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 (~484.78 mM)
Ethanol : ~100 mg/mL (~484.78 mM) H2O : ~1 mg/mL (~4.85 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.12 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 (12.12 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 (12.12 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: ≥ 2.5 mg/mL (12.12 mM) (saturation unknown) in 10% EtOH + 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 EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix well. 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 5: 10% EtOH + 90% Corn Oil Solubility in Formulation 6: 6.67 mg/mL (32.33 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
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 |
| NCT00812422 | COMPLETED | Drug: Dexibuprofen Drug: Dexibuprofen Drug: Ibuprofen |
Fever Respiratory Tract Infection |
Inje University | 2008-02 | Phase 3 |
| NCT02956512 | COMPLETED | Drug: Dexibuprofen | Healthy Volunteers | Apsen Farmaceutica S.A. | 2019-03-18 | Phase 1 |
| NCT02956525 | COMPLETED | Drug: Dexibuprofen | Healthy Volunteers | Apsen Farmaceutica S.A. | 2018-04-01 | Phase 1 |
| NCT01066676 | COMPLETED | Drug: Dexibuprofen Drug: Ibuprofen |
Osteoarthritis of the Hip or Knee | Gebro Pharma GmbH | 2009-10 | Phase 4 |
| NCT01638962 | COMPLETED | Drug: Instruction on analgesic use for pain relief (acetaminophen and NSAIDs) Other: Neuromuscular exercise |
Osteoarthritis, Knee | University of Southern Denmark | 2012-08 | Not Applicable |
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