PD-166793

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PD-166793是一种有效，选择性和具有口服活性的 MMP 的广谱抑制剂，对 MMP-2，MMP-3 和 MMP-13 表现出纳摩尔浓度的效价 (IC50=4，7，8 nM)，对 MMP-1，-7 和 -9 表现出微摩尔的效价 (IC50=6.0，7.2，7.9 μM)。PD-166793 可以减轻进行性心力衰竭的大鼠模型中的左心室重构和功能障碍。

PD-166793 is a potent, selective, orally active and wide‐broad spectrum inhibitor of MMP, exhibiting nanomolar potency against MMP-2, MMP-3 and MMP-13 (IC50=4, 7, and 8 nM, respectively) and micromolar potency vs MMP-1, -7 and -9 (IC50=6.0, 7.2, and 7.9 μM, respectively). PD-166793 can attenuate left ventricular remodeling and dysfunction in a rat model of progressive heart failure.

PD-166793 (0.1 μM) leads to a 20% inhibition of AMP deaminase (AMPD) activity in rat heart homogenates.PD-166793 (100 μM; 36 h) significantly reduces MMP‐9 activity in normal human cardiac fibroblasts.

PD-166793 (1 mg/kg/d; daily gavage for 10 weeks) largely prevents the adverse remodeling characteristically seen in the aortocaval (AV) fistula model.PD-166793 (5 mg/kg; oral gavage) exhibits superior pharmacokinetics (t1/2=43.6 h, Cmax=42.4 μg/mL, AUC0-∞=2822 μg?h/mL) in rats.Animal Model:Male Sprague-Dawley rats (6 weeks) were induced chronic biventricular volume overload Dosage:1 mg/kg Administration:Daily gavage beginning 2 weeks before surgery and continued until 8 weeks after surgery Result:Prevented ventricular dilatation and attenuated the hypertrophy typically induced by chronic volume overload.

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Metabolic Enzyme/Protease

MMP

MMP

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199850-67-4

412.3

C17H18BrNO4S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (242.54 mM; 超声助溶 )

CC(C)[C@H](NS(=O)(=O)c1ccc(cc1)-c1ccc(Br)cc1)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years