DuP-697

Research use only, not for human use.

DuP-697 is an irreversible, specific COX-2 inhibitor with IC50 values of 10 nM and 800 nM for human COX-2 and COX-1. DuP-697 also exhibits anti-angiogenic, anti-inflammatory, antipyretic and apoptotic effects.

DuP-697 is a member of the vicinal diaryl heterocycles and a potent, irreversible, selective and orally active COX-2 inhibitor (IC50 of 10 nM and 800 nM for human COX-2 and COX-1, respectively). DuP-697 exerts antiproliferative (IC50 of 42.8 nM), antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. DuP-697 inhibits prostaglandin synthesis and has anti-inflammatory, anticancer and antipyretic effects.

DuP-697 (0-100 nM; 24 hours; HT29 cells) treatment shows antiproliferative with an IC50 value of 42.8 nM.DuP-697 (25-100 nM; 72 hours; HT29 cells) treatment causes concentration dependent apoptosis in HT29 cells. The percentage of UR (apoptosis portion) area increases gradually according to the concentration of DuP-697 from 7% in control group to 52% in 100 nM DuP-697.DuP-697 in 100, 10 and 1 nM concentrations cause antiangiogenic effect. Antiangiogenic scores of DuP-697 are 1.2, 0.8 and 0.5, respectively.Cell Proliferation Assay Cell Line:HT29 cells Concentration:0 nM, 12.5 nM, 25 nM, 50 nM, 100 nM Incubation Time:24 hours Result:Exhibited decreasing CI values in a concentration dependent manner. Showed statistically significant cytotoxic effect.Apoptosis Analysis Cell Line:HT29 cells Concentration:25 nM, 50 nM, 100 nM Incubation Time:72 hours Result:Caused concentration dependent apoptosis in HT29 cells.

DuP-697 is a potent inhibitor of paw swelling in nonestablished and established adjuvant arthritis in rats (ED50 = 0.03 and 0.18 mg/kg/day, respectively). DuP-697 has no effect on phenylquinone writhing in rats (ED50 greater than 100 mg/kg), but is analgetic against inflammation-related pain in the Randall-Selitto assay (ED50 = 3.5 mg/kg) and is a very potent antipyretic agent (ED50 = 0.05 mg/kg). DuP-697 (5 mg/kg i.v.) does not alter renal blood flow or the renal vascular response to angiotensin II in furosemide-pretreated, volume-depleted rats.DuP-697 is a moderate inhibitor of bull seminal vesicle prostaglandin (PG) synthesis (IC50 of 24 μM) and a potent inhibitor of rat brain PG synthesis (IC50 of 4.5 μM) but was ineffective against rat kidney PG synthesis (IC50 of 75 μM).

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Chromatin/Epigenetic

COX

COX

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88149-94-4

411.31

C17H12BrFO2S2

>98% (HPLC)

In Vitro:?DMF : ≥ 54 mg/mL (131.29 mM) DMSO : ≥ 15 mg/mL (36.47 mM) Ethanol : ≥ 7 mg/mL (17.02 mM)

CS(=O)(=O)c1ccc(cc1)-c1cc(Br)sc1-c1ccc(F)cc1

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(-20℃)

With Ice Pack

≥ 2 years