3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE Basic information
- Product Name:
- 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
- Synonyms:
-
- 3-(4-methylsulfonylphenyl)-4-phenyl-5-(trifluoromethyl)-1,2-oxazole
- CAY10404
- 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
- Isoxazole, 3-[4-(methylsulfonyl)phenyl]-4-phenyl-5-(trifluoromethyl)-
- 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T
- Bcl-XL,CAY10404,cancer,COX,anti-inflammatory,Bcl-2,Apoptosis,Akt,H-1703,Cyclooxygenase,NSCLC,CAY 10404,H-358,inhibit,cell,pGSK-3β,H-460,analgesic,MAPK,CAY-10404,cyclooxygenase-2,lung,anti-cancer,Inhibitor,Non-small,Protein kinase B,pAkt,PKB
- CAY10404, 10 mM in DMSO
- CAS:
- 340267-36-9
- MF:
- C17H12F3NO3S
- MW:
- 367.34
- Mol File:
- Mol File
3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO:100.0(Max Conc. mg/mL);272.23(Max Conc. mM)
- form
- A crystalline solid
- color
- White to off-white
3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE Usage And Synthesis
Uses
CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities[1][2][3].
Definition
ChEBI: Isoxazole, 3-[4-(methylsulfonyl)phenyl]-4-phenyl-5-(trifluoromethyl)- is a sulfonic acid derivative.
in vivo
CAY10404 (50 mg/kg/day; ip; for 4 days) decreases lung inflammation in HTV mice and attenuates ventilator-induced lung injury[2].
| Animal Model: | Adult male C57Bl/6J mice weighing 24-30 g[2] |
| Dosage: | 50 mg/kg |
| Administration: | IP; daily; for 4 days |
| Result: | Attenuated cyclooxygenase activity, significantly decreasing BAL PGE2 and 6-keto PGF1α. Decreased lung inflammation in HTV mice (high tidal volume; 20 ml/kg; for 4 hours) and attenuates ventilator-induced lung injury. |
IC 50
COX-2: 1 nM (IC50); COX-1: >500 μM (IC50)
References
[1] A G Habeeb, et al. Design and synthesis of 4,5-diphenyl-4-isoxazolines: novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity. J Med Chem. 2001 Aug 30;44(18):2921-7. DOI:10.1021/jm0101287
[2] Joshua A Robertson, et al. The role of cyclooxygenase-2 in mechanical ventilation-induced lung injury. Am J Respir Cell Mol Biol. 2012 Sep;47(3):387-94. DOI:10.1165/rcmb.2011-0005OC
[3] Yongseon Cho, et al. Effects of CAY10404 on the PKB/Akt and MAPK pathway and apoptosis in non-small cell lung cancer cells. Respirology. 2009 Aug;14(6):850-8. DOI:10.1111/j.1440-1843.2009.01563.x
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