E-6087
E-6087 is a cyclooxygenase 2 (COX-2) inhibitor potentially for the treatment of osteoarthritis and pain. E-6087 significantly enhanced the response to radiation, reducing mean volume to 32% of tumors treated with radiation only. The combination treatment neither increased apoptosis of tumor cells or stromal cells nor affected tumor microvascular density. In vitro, E-6087 and its active metabolite did not affect clonogenic survival of GL261 cells or human umbilical vein endothelial cell after radiation. In vivo, however, there was a nonsignificant increase in Angiopoietin (Ang)-1 and Tie-2 mRNA levels and a decrease of Ang-2 mRNA levels after combination treatment.
1: Salgado L, Encina G, Farran R, Puig S, Martínez L. Enantioselective HPLC determination of E-6087, a new COX-2 inhibitor, in human plasma: Validation and pharmacokinetic application. Chirality. 2004 May 15;16(5):302-8. PubMed PMID: 15069660.
2: Reinoso RF, Farrán R, Moragon T, García-Soret A, Martínez L. Development and validation of two chromatographic methods for the quantification of E-6087 and one of its metabolites, E-6132, in rat plasma. J Pharm Biomed Anal. 2001 Mar;24(5-6):897-911. PubMed PMID: 11248483.
3: Reinoso RF, Farrán R, Moragón T, García-Soret A, Martínez L. Pharmacokinetics of E-6087, a new anti-inflammatory agent, in rats and dogs. Biopharm Drug Dispos. 2001 Sep;22(6):231-42. PubMed PMID: 11754039.
4: Wagemakers M, van der Wal GE, Cuberes R, Alvarez I, Andrés EM, Buxens J, Vela JM, Moorlag H, Mooij JJ, Molema G. COX-2 Inhibition Combined with Radiation Reduces Orthotopic Glioma Outgrowth by Targeting the Tumor Vasculature. Transl Oncol. 2009 Mar;2(1):1-7. PubMed PMID: 19252746; PubMed Central PMCID: PMC2647697.
5: Pérez-Maseda C, Calvet C, Cuberes R, Frigola J. Determination of enantiomeric purity of a novel COX-2 anti-inflammatory drug by capillary electrophoresis using single and dual cyclodextrin systems. Electrophoresis. 2003 May;24(9):1416-21. PubMed PMID: 12731028.
6: Iñiguez MA, Punzón C, Cacheiro-Llaguno C, Díaz-Muñoz MD, Duque J, Cuberes R, Alvarez I, Andrés EM, Buxens J, Buschmann H, Vela JM, Fresno M. Cyclooxygenase-independent inhibitory effects on T cell activation of novel 4,5-dihydro-3 trifluoromethyl pyrazole cyclooxygenase-2 inhibitors. Int Immunopharmacol. 2010 Oct;10(10):1295-304. doi: 10.1016/j.intimp.2010.07.013. PubMed PMID: 20709632.
7: Calvet C, Cuberes R, Pérez-Maseda C, Frigola J. Enantioseparation of novel COX-2 anti-inflammatory drugs by capillary electrophoresis using single and dual cyclodextrin systems. Electrophoresis. 2002 Jun;23(11):1702-8. PubMed PMID: 12179991.
2: Reinoso RF, Farrán R, Moragon T, García-Soret A, Martínez L. Development and validation of two chromatographic methods for the quantification of E-6087 and one of its metabolites, E-6132, in rat plasma. J Pharm Biomed Anal. 2001 Mar;24(5-6):897-911. PubMed PMID: 11248483.
3: Reinoso RF, Farrán R, Moragón T, García-Soret A, Martínez L. Pharmacokinetics of E-6087, a new anti-inflammatory agent, in rats and dogs. Biopharm Drug Dispos. 2001 Sep;22(6):231-42. PubMed PMID: 11754039.
4: Wagemakers M, van der Wal GE, Cuberes R, Alvarez I, Andrés EM, Buxens J, Vela JM, Moorlag H, Mooij JJ, Molema G. COX-2 Inhibition Combined with Radiation Reduces Orthotopic Glioma Outgrowth by Targeting the Tumor Vasculature. Transl Oncol. 2009 Mar;2(1):1-7. PubMed PMID: 19252746; PubMed Central PMCID: PMC2647697.
5: Pérez-Maseda C, Calvet C, Cuberes R, Frigola J. Determination of enantiomeric purity of a novel COX-2 anti-inflammatory drug by capillary electrophoresis using single and dual cyclodextrin systems. Electrophoresis. 2003 May;24(9):1416-21. PubMed PMID: 12731028.
6: Iñiguez MA, Punzón C, Cacheiro-Llaguno C, Díaz-Muñoz MD, Duque J, Cuberes R, Alvarez I, Andrés EM, Buxens J, Buschmann H, Vela JM, Fresno M. Cyclooxygenase-independent inhibitory effects on T cell activation of novel 4,5-dihydro-3 trifluoromethyl pyrazole cyclooxygenase-2 inhibitors. Int Immunopharmacol. 2010 Oct;10(10):1295-304. doi: 10.1016/j.intimp.2010.07.013. PubMed PMID: 20709632.
7: Calvet C, Cuberes R, Pérez-Maseda C, Frigola J. Enantioseparation of novel COX-2 anti-inflammatory drugs by capillary electrophoresis using single and dual cyclodextrin systems. Electrophoresis. 2002 Jun;23(11):1702-8. PubMed PMID: 12179991.
| Chemical | |
|---|---|
| CAS Num | 251442-94-1 |
| Chemical Formula | C16H12F5N3O2S |
| Molecular Weight | 405.343 |
| IUPAC Chemical Name | 4-(5-(2,4-difluorophenyl)-3-(trifluoromethyl)-4,5-dihydro-1H-pyrazol-1-yl)benzenesulfonamide |
| Exact Mass | 405.057 |
| Elemental Analysis | C, 47.41; H, 2.98; F, 23.43; N, 10.37; O, 7.89; S, 7.91 |
| Synonym | E-6087; E 6087; E6087 |
| Solubility | Soluble in DMSO |
| SMILES Code | O=S(C1=CC=C(N2N=C(C(F)(F)F)CC2C3=CC=C(F)C=C3F)C=C1)(N)=O |
| Biological | |
| Targets and Effects | COX-2 inhibitor |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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