CAS NO: | 188817-13-2 |
生物活性 | SC-560 is a potent and selectiveCOX-1inhibitor with anIC50of 9 nM. | ||||||||||||||||
IC50& Target |
| ||||||||||||||||
体外研究 (In Vitro) | Preincubation of COX-1 with SC-560 inhibits the conversion of arachidonic acid to PGE2 in a concentration-dependent manner. The IC50of SC-560 for COX-2 is 6.3 μM, nearly 1,000-fold higher than with COX-1[1]. SC-560 shows a dose and time dependent inhibitory effect on HCC cell growth. SC-560 also inhibits colony formation in soft agar and induces apoptosis in HCC cells in a dose-dependent manner. Moreover, SC-560 decreases the levels of the anti-apoptotic proteins survivin and XIAP and activates caspase 3 and 7 in a dose and time dependent fashion[2]. | ||||||||||||||||
体内研究 (In Vivo) | Oral dosing with either 10 or 30 mg/kg SC-560 1 hour before assay completely inhibits ionophore-stimulated TxB2production, indicating that SC-560 is orally bioavailable and inhibits COX-1in vivo[1]. SC-560 extensively distributes into rat tissues, and has a CL approaching hepatic plasma flow. The drug displays low less than 15% and formulation dependent bioavailability after oral administration and demonstrates kidney toxicity[3]. | ||||||||||||||||
分子量 | 352.74 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C17H12ClF3N2O | ||||||||||||||||
CAS 号 | 188817-13-2 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
| ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 100 mg/mL(283.49 mM;Need ultrasonic) 配制储备液
* 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。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
|
维奥蛋白资源库 - 中文蛋白资源 CopyRight © 2010-2024 |