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340267-36-9

中文名稱 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
英文名稱 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
CAS 340267-36-9
分子式 C17H12F3NO3S
分子量 367.34
MOL 文件 340267-36-9.mol
更新日期 2024/12/23 17:39:04
340267-36-9 結(jié)構(gòu)式 340267-36-9 結(jié)構(gòu)式

基本信息

中文別名
化合物CAY10404
英文別名
CAY10404
3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
3-(4-methylsulfonylphenyl)-4-phenyl-5-(trifluoromethyl)-1,2-oxazole
Isoxazole, 3-[4-(methylsulfonyl)phenyl]-4-phenyl-5-(trifluoromethyl)-

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
溶解度DMSO:100.0(Max Conc. mg/mL);272.23(Max Conc. mM)
形態(tài)結(jié)晶固體
顏色White to off-white
3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-1215373-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
CAY10404
340267-36-95mg900元
2024/11/08HY-1215373-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
CAY10404
340267-36-910mM * 1mLin DMSO990元
2024/11/08HY-1215373-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-TRIFLUOROMETHYLISOXAZOLE
CAY10404
340267-36-910mg1500元

常見問題列表

生物活性
CAY10404 是一種有效且高度選擇性的環(huán)氧合酶 2 (COX-2) 抑制劑,IC50 為 1 nM,選擇性指數(shù) (SI;COX-1 IC50/COX-2 IC50) 為 >500000。CAY10404 是有效的 PKB/Akt 和 MAPK 信號通路抑制劑,可誘導(dǎo)非小細(xì)胞肺癌 (NSCLC) 細(xì)胞凋亡 (apoptosis)。CAY10404 是一種二芳基異惡唑,具有良好的止痛,抗炎和抗癌活性。
靶點

COX-2

1 nM (IC 50 )

COX-1

>500 μM (IC 50 )

Akt

體外研究

CAY10404 (compound 7) exhibits no inhibition of COX-1 (IC 50 >500 μM).
CAY10404 (10-100 μM; for 3 days) inhibits the growth of NSCLC cell lines in a concentration-dependent manner and has an average 50% inhibitory concentration (IC 50 ) of 60-100 μM.
CAY10404 (20-100 μM; for 3 days) induces apoptosis in NSCLC cells.
CAY10404 (80 μM; for 3 days) induces a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-X L ) and pAkt and pGSK-3β.
CAY10404 (20, 50, 80, 100 μM; for 14 days) compromises the ability of H460 cells to form colonies in anchorage-independent growth in a concentration-dependent manner.

Cell Viability Assay

Cell Line: Non-small cell lung cancer (NSCLC) cells (H1703, H358, H460)
Concentration: 10-100 μM
Incubation Time: For 3 days
Result: Inhibited the growth of NSCLC cell lines in a concentration-dependent manner.

Apoptosis Analysis

Cell Line: H460 cells
Concentration: 20, 50, 100 μM
Incubation Time: For 3 days
Result: Induced apoptosis.

Western Blot Analysis

Cell Line: NSCLC cells (H358, H460)
Concentration: 80 μM
Incubation Time: For 3 days
Result: Induced a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-X L ) and pAkt and pGSK-3β, without changing the level of the pro-apoptotic protein (Bax) and total Akt and GSK-3β protein levels.
體內(nèi)研究

CAY10404 (50 mg/kg/day; ip; for 4 days) decreases lung inflammation in HTV mice and attenuates ventilator-induced lung injury.

Animal Model: Adult male C57Bl/6J mice weighing 24-30 g
Dosage: 50 mg/kg
Administration: IP; daily; for 4 days
Result: Attenuated cyclooxygenase activity, significantly decreasing BAL PGE2 and 6-keto PGF1α.
Decreased lung inflammation in HTV mice (high tidal volume; 20 ml/kg; for 4 hours) and attenuates ventilator-induced lung injury.
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