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XL-784 free base

CAS No. : 1356992-21-6

MCE 站：XL-784 free base

产品活性：XL-784 free base 是 MMP 的一个选择性抑制剂，其对 MMP-1，MMP-3，MMP-8，MMP-9，MMP-13 的 IC₅₀ 值分别约为 1900，0.81，120，10.8，18，0.56 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：MMP

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, andADAM10 [TNF-α-converting enzyme (TACE)] activity in vitro, with IC₅₀ values 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).

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%; all Ps<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.

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