Enflicoxib

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Chemical Information

Product name：Enflicoxib	Purity：98% min
CAS NO：251442-94-1	Solubility：
Molecular Formula：C₁₆H₁₂F₅N₃O₂S	Package：Package according to customer requirements
Molecular Weight：405.3 g/mol	Storage：-20 ℃

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Remarks

Enflicoxib, also known as 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

References

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.