5-溴-2-（4-氟苯基）-3-（4-甲基磺酰基苯基）噻吩
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- CAS号:
- 88149-94-4
- 英文名:
- DUP-697
- 英文别名:
- BFMeT;DUP-697;DuP697,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]-
- 中文名:
- 5-溴-2-（4-氟苯基）-3-（4-甲基磺酰基苯基）噻吩
- 中文别名:
- 化合物 T15181;DUP 697,环氧合酶2(COX-2)抑制剂;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
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5-溴-2-（4-氟苯基）-3-（4-甲基磺酰基苯基）噻吩化学性质
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储存条件:
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2-8°C
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溶解度:
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DMF: 54 mg/ml; DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml; DMSO: 15 mg/ml; Ethanol: 7 mg/ml
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形态:
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White to off-white solid.
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颜色:
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White to off-white
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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
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。
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hCOX-2
10 nM (IC
50
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hCOX-1
800 nM (IC
50
)
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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
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Cell Line:
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HT29 cells
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Concentration:
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0 nM, 12.5 nM, 25 nM, 50 nM, 100 nM
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Incubation Time:
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24 hours
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Result:
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Exhibited decreasing CI values in a concentration dependent manner. Showed statistically significant cytotoxic effect.
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Apoptosis Analysis
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Cell Line:
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HT29 cells
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Concentration:
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25 nM, 50 nM, 100 nM
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Incubation Time:
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72 hours
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Result:
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Caused concentration dependent apoptosis in HT29 cells.
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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).
5-溴-2-（4-氟苯基）-3-（4-甲基磺酰基苯基）噻吩
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/08/19 | HY-103387 | DuP-697 | | 1 mg | 1000元 |
| 2024/08/19 | HY-103387 | DuP-697 | | 5 mg | 2000元 |
5-溴-2-（4-氟苯基）-3-（4-甲基磺酰基苯基）噻吩
生产厂家
88149-94-4, 5-溴-2-（4-氟苯基）-3-（4-甲基磺酰基苯基）噻吩 相关搜索:
- API intermediates
- Lipid signaling
- 酶
- 医药中间体
- C17H12BrFO2S2
- DUP 697,环氧合酶2(COX-2)抑制剂
- 化合物 T15181
- 5-溴-2-(4-氟苯基)-3-(4-甲基磺酰基苯基)噻吩
- 88149-94-4
- DuP697,DuP 697
- Thiophene, 5-bromo-2-(4-fluorophenyl)-3-[4-(methylsulfonyl)phenyl]-
- DuP-697 Assay Reagent
- BFMeT
- 5-BROMO-2-(4-FLUOROPHENYL)-3-(4-(METHYLSULFONYL)PHENYL)THIOPHENE
- DUP-697