产品
编 号：F247248
分子式：C17H18BrNO4S
分子量：412.3
分子式：C17H18BrNO4S
分子量：412.3
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 199850-67-4
产品详情
生物活性：
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.
体内研究：
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.
体外研究：
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 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.
体内研究：
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.
体外研究：
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.
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