DUP-697

Description

DuP-697 is a member of the diaryl heterocycle group of selective COX-2 inhibitors which includes MK-966 (rofecoxib), SC-58125, and celecoxib. DuP-697 is a potent and time-dependent inhibitor of COX-2. When tested on isolated recombinant enzymes, DuP-697 is at least 50 times more potent in the inhibition of COX-2 than COX-1. The IC₅₀ values for human recombinant COX-2 are 80 and 40 nM at 5 and 10 minutes, respectively. The IC₅₀ for the inhibition of human recombinant COX-1 after the same time intervals is 9 μM. DuP-697 also attenuates the COX-1 inhibitory activity of non-selective COX inhibitors such as indomethacin.

Uses

DuP-697 is a thiophene that inhibits COX-2 and acts as a NSAID.

Definition

ChEBI: DuP 697 is a member of thiophenes.

Biological Activity

Potent and selective inhibitor of cyclooxygenase-2 (IC 50 values are 10 and 800 nM for COX-2 and COX-1 respectively). Inhibits prostaglandin synthesis and is anti-inflammatory in vivo . Orally active.

storage

Store at +4°C

References

[1] STACIA KARGMAN. Mechanism of selective inhibition of human prostaglandin G/H synthase-1 and -2 in intact cells[J]. Biochemical pharmacology, 1996, 52 7: Pages 1113-1125. DOI: 10.1016/0006-2952(96)00462-5
[2] K SEIBERT. Pharmacological manipulation of cyclo-oxygenase-2 in the inflamed hydronephrotic kidney.[J]. British Journal of Pharmacology, 1996, 117 6: 1016-1020. DOI: 10.1111/j.1476-5381.1996.tb16691.x
[3] MOTI ROSENSTOCK  Gilad R  Abraham Danon. PGHS-2 inhibitors, NS-398 and DuP-697, attenuate the inhibition of PGHS-1 by aspirin and indomethacin without altering its activity[J]. Biochimica et biophysica acta. Molecular and cell biology of lipids, 1999, 1440 1: Pages 127-137. DOI: 10.1016/s1388-1981(99)00105-5