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PD-166793

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Chemical Structure| 199850-67-4 同义名 : -
CAS号 : 199850-67-4
货号 : A395571
分子式 : C17H18BrNO4S
纯度 : 95%
分子量 : 412.298
MDL号 : MFCD09038565
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(254.67 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 PD-166793 is a potent, selective, orally active, pan-MMP inhibitor with IC50 values of 4, 7, and 8 nM for MMP-2, MMP-3, and MMP-13, respectively, and 6.0, 7.2, and 7.9 μM for MMP-1, -7, and -9, respectively. PD-166793 reduces left ventricular remodeling and dysfunction in rat models of progressive heart failure[1][2][3].PD-166793 inhibited AMPD activity in rat heart homogenates by 20% at a concentration of 0.1 μM, and significantly reduced MMP-9 activity in normal human cardiac fibroblasts at a concentration of 100 μM for 36 h[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.43mL

0.49mL

0.24mL

12.13mL

2.43mL

1.21mL

24.25mL

4.85mL

2.43mL
参考文献

[1]O'Brien PM, et, al. Structure-activity relationships and pharmacokinetic analysis for a series of potent, systemically available biphenylsulfonamide matrix metalloproteinase inhibitors. J Med Chem. 2000 Jan 27;43(2):156-66.

[2]Kaludercic N, et, al. Inhibiting metalloproteases with PD 166793 in heart failure: impact on cardiac remodeling and beyond. Cardiovasc Ther. Spring 2008;26(1):24-37.

[3]Chancey AL, et, al. Effects of matrix metalloproteinase inhibition on ventricular remodeling due to volume overload. Circulation. 2002 Apr 23;105(16):1983-8.