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DuP-697

CAS No. : 88149-94-4

MCE 站：DuP-697

产品活性：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。

研究领域：Immunology/Inflammation  |  Apoptosis

作用靶点：COX  |  Apoptosis

In Vitro: 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.

In Vivo: DuP-697 is a potent inhibitor of paw swelling in stablished and established adjuvant arthritis in rats (ED₅₀ = 0.03 and 0.18 mg/kg/day, respectively). DuP-697 has no effect on phenylqui 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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