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PD-166793 {[allProObj[0].p_purity_real_show]}

货号:A395571 Ambeed 开学季,买赠积分,赢豪礼

Broad spectrum MMP inhibitor

PD-166793 化学结构 CAS号:199850-67-4
PD-166793 化学结构
CAS号:199850-67-4
PD-166793 3D分子结构
CAS号:199850-67-4
PD-166793 化学结构 CAS号:199850-67-4
PD-166793 3D分子结构 CAS号:199850-67-4
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PD-166793 纯度/质量文件 产品仅供科研

货号:A395571 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 MMP 其他靶点 纯度
Marimastat +++

MMP-14, IC50: 3 nM

MMP-7, IC50: 16 nM

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Ilomastat ++++

MMP-26, Ki: 0.36 nM

MMP-2, Ki: 0.1 nM

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SB-3CT +

MMP-9, Ki: 600 nM

MMP-2, Ki: 13.9 nM

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Doxycycline {[allProObj[0].p_purity_real_show]}
Batimastat +++

MMP-1, IC50: 3 nM

MMP-7, IC50: 4 nM

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Nobiletin {[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

PD-166793 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].

PD-166793 动物研究

Animal study At a dose of 1 mg/kg/day administered by gavage daily for 10 weeks, PD-166793 largely prevented the adverse remodelling commonly seen in the aortocaval (AV) fistula model[3].Administered orally at a dose of 5 mg/kg, PD-166793 exhibited excellent pharmacokinetics in rats with a t1/2 of 43.6 hours, Cmax of 42.4 μg/mL, and an AUC0-∞ of 2,822 μg/hour/mL[1].Administered daily by gavage at a dose of 1 mg/kg, starting 2 weeks before surgery and continuing until 8 weeks after surgery, PD-166793 prevents ventricular dilatation and attenuates typical hypertrophy caused by chronic volume overload in animals[3].

PD-166793 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.

PD-166793 实验方案

计算器
存储液制备 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

PD-166793 技术信息

CAS号199850-67-4
分子式C17H18BrNO4S
分子量 412.298
别名
运输蓝冰
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
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