5-溴-2-（4-氟苯基）-3-（4-甲基磺酰基苯基）噻吩
- CAS号:88149-94-4
- 英文名:DUP-697
- 中文名:5-溴-2-（4-氟苯基）-3-（4-甲基磺酰基苯基）噻吩
- CBNumber:CB8397180
- 分子式:C17H12BrFO2S2
- 分子量:411.31
- MOL File:88149-94-4.mol
- 储存条件 :2-8°C
- 溶解度 :DMF: 54 mg/ml; DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml; DMSO: 15 mg/ml; Ethanol: 7 mg/ml
- 形态 :White to off-white solid.
- 颜色 :White to off-white
5-溴-2-（4-氟苯基）-3-（4-甲基磺酰基苯基）噻吩性质、用途与生产工艺
- 生物活性 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。
-
靶点
hCOX-2
10 nM (IC 50 )
hCOX-1
800 nM (IC 50 )
-
体外研究
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. -
体内研究
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).
- 更新日期：2024/11/08
- 产品编号：HY-103387
- 产品名称：DuP-697
- CAS编号：
- 包装：1 mg
- 价格：450元
- 更新日期：2024/11/08
- 产品编号：HY-103387
- 产品名称：DuP-697
- CAS编号：
- 包装：5 mg
- 价格：990元
- 公司名称：SIGMA
- 联系电话：--
- 电子邮件：
- 国家：瑞士
- 产品数：6896
- 优势度：91
