N-[(4'-溴[1,1'-联苯]-4-基)磺酰基]-L-缬氨酸
中文名称 | N-[(4'-溴[1,1'-联苯]-4-基)磺酰基]-L-缬氨酸 |
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中文同义词 | (S)-2-(4'-溴-[1,1'-联苯]-4-基磺酰胺O)-3-甲基丁酸;N-[(4'-溴[1,1'-联苯]-4-基)磺酰基]-L-缬氨酸;(S)-2-(4'-溴联苯-4-磺酰胺)-3-甲基丁酸;化合物 T20563;(S)-2-(4'-溴-[1,1'-联苯]-4-基磺酰胺基)-3-甲基丁酸;PD 166793,广谱MMP抑制剂 |
英文名称 | PD 166793 |
英文同义词 | PD 166793;(S)-2-(4'-bromobiphenyl-4-ylsulfonamido)-3-methylbutanoic acid;N-[(4'-Bromo[1,1'-biphenyl]-4-yl)sulfonyl]-L-valine;(S)-2-(4'-Bromo-[1,1'-biphenyl]-4-ylsulfonamido)-3-methylbutanoic acid;MMP-2/MMP-3 Inhibitor;L-Valine, N-[(4'-bromo[1,1'-biphenyl]-4-yl)sulfonyl]-;(2S)-2-[[4-(4-bromophenyl)phenyl]sulfonylamino]-3-methylbutanoicaci;PD 166793 USP/EP/BP |
CAS号 | 199850-67-4 |
分子式 | C17H18BrNO4S |
分子量 | 412.3 |
EINECS号 | |
相关类别 | Angiogenesis and Metastasis;Protease inhibitor |
Mol文件 | 199850-67-4.mol |
结构式 |
N-[(4'-溴[1,1'-联苯]-4-基)磺酰基]-L-缬氨酸 性质
熔点 | 192-193℃ |
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密度 | 1.457 |
储存条件 | Sealed in dry,2-8°C |
溶解度 | DMF:50mg/mL; DMSO:50mg/mL; DMSO:PBS (pH 7.2) (1:1):0.5 mg/ml;乙醇:10mg/mL |
形态 | 结晶固体 |
颜色 | 白至粉红 |
MMP-2 4 nM (IC 50 ) |
MMP-3 7 nM (IC 50 ) |
MMP-13 8 nM (IC 50 ) |
MMP-1 6.0 μM (IC 50 ) |
MMP-7 7.2 μM (IC 50 ) |
MMP-9 7.9 μM (IC 50 ) |
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 (t
1/2
=43.6 h, C
max
=42.4 µg/mL, AUC
0-∞
=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. |
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-107428 | N-[(4'-溴[1,1'-联苯]-4-基)磺酰基]-L-缬氨酸 PD-166793 | 199850-67-4 | 5mg | 1100元 |
2024/08/19 | HY-107428 | PD-166793 | 10 mM * 1 mLin DMSO | 1210元 |