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CAY10404  ≥98%

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包装规格：5mg 10mg in glass bottle
溶解性：溶于DMSO（100 mg/mL 超声）
产品描述：基本信息 产品编号： C10838 产品名称： CAY10404 CAS: 340267-36-9   储存条件 粉末 -20℃ 四年     分子式： C17H12F3NO3S 溶于液体 -80℃ 两年 分子量 367.34 -20℃ 一个月 化学名：  3-[4-(Methylsulfonyl)phenyl]-4-phenyl-5-(trifluoromethyl)-isoxazole Solubility (25°C)：   体外:   DMSO 100mg/mL(272.23mM;Need ultrasonic) Ethanol   Water   体内(现配现用): 1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline，Solubility:2.5mg/mL(6.81mM);Suspended solution; Need ultrasonic 此⽅案可获得2.5mg/mL(6.81mM)的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射。以1mL⼯作液为例，取100μL25.0mg/mL的澄清DMSO储备液加到400μLPEG300中，混合均匀；向上述体系中加⼊50μLTween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。 2.请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in saline) Solubility:2.5mg/mL(6.81mM);Suspended solution; Need ultrasonic 此⽅案可获得2.5mg/mL(6.81mM)的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射。以1mL⼯作液为例，取100μL25.0mg/mL的澄清DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶液中，混合均匀。 3.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility:≥2.5mg/mL(6.81mM);Clear solution 此⽅案可获得≥2.5mg/mL(6.81mM，饱和度未知)的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例，取100μL25.0mg/mL的澄清DMSO储备液加到900μL⽟⽶油中，混合均匀。 ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.7223mL 13.6114mL 27.2227mL 5mM 0.5445mL 2.7223mL 5.4445mL 10mM 0.2722mL 1.3611mL 2.7223mL 生物活性 产品描述 一种有效且高度选择性的环氧合酶2(COX-2)抑制剂，IC50为1nM，选择性指数(SI；COX-1IC50/COX-2IC50)为>500000。 靶点 COX-2 1nM(IC50) COX-1 >500μM(IC50) Akt 体外研究 CAY10404 (compound 7) exhibits no inhibition of COX-1 (IC50>500µM) CAY10404 (10-100µM; for 3 days) inhibits the growth of NSCLC cell lines in a concentration-dependent manner and has an average 50% inhibitory concentration (IC50) of 60-100µM CAY10404 (20-100µM; for 3 days) induces apoptosis in NSCLC cells CAY10404 (80µM; for 3 days) induces a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-XL) and pAkt and pGSK-3β CAY10404 (20, 50, 80, 100µM; 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: 10-100µM 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, 100µM Incubation Time: For 3 days Result: Induced apoptosis. Western Blot Analysis Cell Line: NSCLC cells (H358, H460) Concentration: 80µM Incubation Time: For 3 days Result: Induced a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-XL) and pAkt and pGSK-3β, without changing the level of the pro-apoptotic protein (Bax) and total Akt and GSK-3β protein levels. 体内研究 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.
保存条件：-20℃

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