5-溴-2-（4-氟苯基）-3-（4-甲基磺?；交┼绶?/span>

生物活性靶點體外研究體內研究 5-溴-2-（4-氟苯基）-3-（4-甲基磺?；交┼绶?試劑級價格

5-溴-2-（4-氟苯基）-3-（4-甲基磺?；交┼绶? 88149-94-4, 結構式

5-溴-2-（4-氟苯基）-3-（4-甲基磺?；交┼绶?/a>

CAS號:: 88149-94-4

英文名:: DUP-697

英文別名:: BFMeT;DUP-697;DuP697,DuP 697;DuP-697 Assay Reagent;DuP-697, 10 mM in DMSO;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?；交┼绶?/dd>

中文別名:: 化合物 T15181;化合物 DUP-697;DUP 697,環(huán)氧合酶2(COX-2)抑制劑;化合物DUP-697,10 MM DMSO 溶液;5-溴-2-(4-氟苯基)-3-(4-甲基磺?；交?噻吩

CBNumber:: CB8397180

分子式:: C17H12BrFO2S2

分子量:: 411.31

MOL File:: 88149-94-4.mol

化學性質安全信息用途價格供應商 82

5-溴-2-（4-氟苯基）-3-（4-甲基磺酰基苯基）噻吩化學性質

儲存條件:: 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

形態(tài):: White to off-white solid.

顏色:: White to off-white

安全信息

危險品標志:	Xi

危險類別碼:	36/37/38

安全說明:	26-36

5-溴-2-（4-氟苯基）-3-（4-甲基磺酰基苯基）噻吩性質、用途與生產工藝

生物活性

DuP-697 是鄰位二芳基雜環(huán)的成員，并且是一種有效，不可逆，選擇性和口服活性的 COX-2 抑制劑 (對于人 COX-2 和 COX-1，IC50 分別為 10 nM 和 800 nM)。DuP-697 對 HT29 大腸癌細胞具有抗增殖作用 (IC50 為 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，抗癌和退燒的作用。

靶點

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.

體內研究

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).