产品描述
DuP-697 is an irreversible and orally active COX-2 inhibitor (IC50: 10 nM and 800 nM for human COX-2 and COX-1) with anti-inflammatory, anticancer, and antipyretic effects. DuP-697 shows antiproliferative (IC50: 42.8 nM), antiangiogenic and apoptotic effects on HT29 colorectal cancer cells.
体外活性
DuP-697 (25-100 nM; 72 hours; HT29 cells) treatment results in concentration dependent apoptosis in HT29 cells. DuP-697 (0-100 nM; 24 hours; HT29 cells) treatment displays antiproliferative (IC50: 42.8 nM). DuP-697 (100nM, 10nM and 1 nM) concentrations cause antiangiogenic effect. 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. Antiangiogenic scores of DuP-697 are 1.2, 0.8 and 0.5, respectively [1].
体内活性
DuP-697 is a moderate inhibitor of bull seminal vesicle prostaglandin (PG) synthesis (IC50 of 24 μM). 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) and it is also a potent inhibitor of rat brain PG synthesis (IC50 of 4.5 μM). However, it was ineffective against rat kidney PG synthesis (IC50 of 75 μM). 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 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) [2].
Cas No.
88149-94-4
分子式
C17H12BrFO2S2
分子量
411.31
别名
DuP-697
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years