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88149-94-4

中文名稱 5-溴-2-(4-氟苯基)-3-(4-甲基磺?;交┼绶?
英文名稱 DUP-697
CAS 88149-94-4
分子式 C17H12BrFO2S2
分子量 411.31
MOL 文件 88149-94-4.mol
更新日期 2024/11/07 22:36:15
88149-94-4 結(jié)構(gòu)式 88149-94-4 結(jié)構(gòu)式

基本信息

中文別名
化合物 T15181
5-溴-2-(4-氟苯基)-3-(4-甲基磺?;交?噻吩
英文別名
BFMeT
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]-

物理化學(xué)性質(zhì)

儲(chǔ)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)白色至類白色固體
顏色White to off-white

安全數(shù)據(jù)

危險(xiǎn)品標(biāo)志Xi
危險(xiǎn)類別碼36/37/38
安全說(shuō)明26-36

常見問題列表

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(duì)于人 COX-2 和 COX-1,IC50 分別為 10 nM 和 800 nM)。DuP-697 對(duì) HT29 大腸癌細(xì)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(diǎn)

hCOX-2

10 nM (IC 50 )

hCOX-1

800 nM (IC 50 )

體外研究

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.
體內(nèi)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).

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