CAS NO: | 1356992-21-6 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | XL-784 free base is a selectivematrix metalloproteinases(MMP)inhibitor, withIC50sof ~1900, 0.81, 120, 10.8, 18, 0.56 nM forMMP-1,MMP-2,MMP-3,MMP-8,MMP-9andMMP-13, respectively[1][2]. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | XL-784 is a highly potent, low-molecular-weight (1,122 g/mol) inhibitor of MMPs that has very limited aqueous solubility (20 μg/mL). XL-784 potently inhibits MMP-2, MMP-13, and ADAM10 [TNF-α-converting enzyme (TACE)] activity in vitro, with IC50values in the range of 1-2 nM. XL-784 also inhibits MMP-9 (IC50~20 nM) activity and ADAM17 (IC50~70 nM) also known as TACE. However, it exhibits low potency for inhibition of MMP-1 (IC50~2,000 nM)[1]. | ||||||||||||||||
体内研究 (In Vivo) | All mice tolerate the treatments similarly. Control mice all developed aneurysms with a mean %△AD of 158.5%±4.3%. Treatment with all doses of XL-784 and doxycycline are effective in inhibiting aortic dilatation. There is a clear dose-response relationship between XL-784 and reductions in aortic dilatation at harvest (50 mg/kg 140.4% ±3.2%; 125 mg/kg 129.3% ±5.1%; 250 mg/kg 119.2%±3.5%; allPs<0.01 compared to control). This continues with the higher doses (375 mg/kg 88.6%±4.4%; 500 mg/kg 76.0%±3.5%). The highest 2 doses of XL-784 tested are more effective than doxycycline (112.2%±2.0%, P<0.05) in inhibiting maximal dilatation of the aorta after elastase perfusion[2]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 549.93 | ||||||||||||||||
Formula | C21H22ClF2N3O8S | ||||||||||||||||
CAS 号 | 1356992-21-6 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 250 mg/mL(454.60 mM;Need ultrasonic) 配制储备液
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
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