| Size | Price | Stock | Qty |
|---|---|---|---|
| 1g |
|
||
| 5g |
|
||
| 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
The time it take to reach peak plasma concentration is 2.25-5 hours post-administration of oral tablets containing 300mg of dexibuprofen. For more information, refer to [ibuprofen]. Mainly renal excretion. For more information, refer to [ibuprofen]. For more information, refer to [ibuprofen]. For more information, refer to [ibuprofen]. Metabolism / Metabolites For more information, refer to [ibuprofen]. (S)-(+)-ibuprofen has known human metabolites that include 2-Hydroxyibuprofen and 3-Hydroxyibuprofen. Biological Half-Life Oral tablets containing 300mg of dexibuprofen results in 2.2-4.7 hours. For more information, refer to [ibuprofen]. |
| Toxicity/Toxicokinetics |
Protein Binding
For more information, refer to [ibuprofen]. |
| References |
|
| Additional Infomation |
Dexibuprofen is an ibuprofen. It has a role as a non-narcotic analgesic and a non-steroidal anti-inflammatory drug. It is an enantiomer of a levibuprofen.
Dexibuprofen, S(+)-ibuprofen, is a non-steroidal anti-inflammatory drug (NSAID). It is a pharmacologically effective enantiomer of racemic ibuprofen that differs in physicochemical properties. It is proposed to be more pharmacologically active and tolerable with a better safety profile than ibuprofen due to higher concentration of active S enantiomer. Dexibuprofen has a slower dissolution rate in the simulated gastric and enteric juices compared with the racemic ibuprofen and displays improved oral bioavilability. For Metabolism, Enzymes, Carriers, Transporters Sections, refer to [Ibuprofen]. See also: Ibuprofen (annotation moved to). Drug Indication For more information, refer to [ibuprofen]. Mechanism of Action Like common NSAIDs, dexibuprofen is an active enantiomer of [ibuprofen] that suppresses the prostanoid synthesis in the inflammatory cells via inhibition of the COX-2 isoform of the arachidonic acid COX. For more information, refer to [ibuprofen]. Pharmacodynamics For more information, 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 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
