DuP-697

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

DuP-697 是邻位二芳基杂环的成员，并且是一种有效，不可逆，选择性和口服活性的 COX-2 抑制剂 (对于人 COX-2 和 COX-1，IC50 分别为 10 nM 和 800 nM)。DuP-697 对 HT29 大肠癌细胞具有抗增殖作用 (IC50 为 42.8 nM)，抗血管生成和促凋亡作用。DuP-697 可抑制前列腺素的合成，并具有抗炎，抗癌和退烧的作用。

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).

——

Chromatin/Epigenetic

COX

COX

——

——

88149-94-4

411.31

C17H12BrFO2S2

>98% (HPLC)

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

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

——

(-20℃)

With Ice Pack

≥ 2 years