COX-2-IN-26

Names

[ CAS No. ]:
2413565-19-0

[ Name ]:
COX-2-IN-26

Biological Activity

[Description]:

COX-2-IN-26 is a potent, selective and orally active COX-2 inhibitor with IC50 values of 10.61, 0.067, 1.96 µM for COX-1, COX-2, 15-LOX, respectively. COX-2-IN-26 shows anti-inflammatory activity. COX-2-IN-26 shows gastrointestinal safety profile[1].

[Related Catalog]:

Research Areas >> Inflammation/Immunology
Signaling Pathways >> Immunology/Inflammation >> COX

[Target]

COX-2:0.067 μM (IC50)

COX-1:10.61 μM (IC50)

15-LOX:1.96 μM (IC50)


[In Vitro]

COX-2-IN-26 (compound 16) shows significant COX-2 selectivity with an SI value of 158.36[1].

[In Vivo]

COX-2-IN-26 (28 µM/kg) shows a potent anti-inflammatory activity in rats with edema inhibition relative to indomethacin of 102% and 119% in 4h and 3h, respectively[1]. .COX-2-IN-26 (10, 30, 50 mg/kg; p.o.) shows GI safety profile with normal appearance for mucosa with intact surface epithelium and preserves glands but there is some congestion of the blood vessels in albino rats[1].

[References]

[1]. Maghraby MT, et al. Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. Bioorg Med Chem. 2020 Apr 1;28(7):115403.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H21N7OS3

[ Molecular Weight ]:
507.65

Related Compounds