88149-94-4
基本信息
5-溴-2-(4-氟苯基)-3-(4-甲基磺?;交?噻吩
DUP-697
DuP-697 Assay Reagent
5-BROMO-2-(4-FLUOROPHENYL)-3-(4-(METHYLSULFONYL)PHENYL)THIOPHENE
Thiophene, 5-bromo-2-(4-fluorophenyl)-3-[4-(methylsulfonyl)phenyl]-
物理化學(xué)性質(zhì)
常見問題列表
hCOX-2 10 nM (IC 50 ) |
hCOX-1 800 nM (IC 50 ) |
DuP-697 (0-100 nM; 24 hours; HT29 cells) treatment shows antiproliferative with an IC
50
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 (ED
50
= 0.03 and 0.18 mg/kg/day, respectively). DuP-697 has no effect on phenylquinone writhing in rats (ED
50
greater than 100 mg/kg), but is analgetic against inflammation-related pain in the Randall-Selitto assay (ED
50
= 3.5 mg/kg) and is a very potent antipyretic agent (ED
50
= 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 (IC
50
of 24 μM) and a potent inhibitor of rat brain PG synthesis (IC
50
of 4.5 μM) but was ineffective against rat kidney PG synthesis (IC
50
of 75 μM).