N-[(4'-溴[1,1'-联苯]-4-基)磺酰基]-L-缬氨酸
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- CAS号:
- 199850-67-4
- 英文名:
- PD 166793
- 英文别名:
- PD 166793;PD-166793-0000;PD 166793 USP/EP/BP;MMP-2/MMP-3 Inhibitor;N-[(4'-Bromo[1,1'-biphenyl]-4-yl)sulfonyl]-L-valine;L-Valine, N-[(4'-bromo[1,1'-biphenyl]-4-yl)sulfonyl]-;(S)-2-(4'-bromobiphenyl-4-ylsulfonamido)-3-methylbutanoic acid;(2S)-2-[[4-(4-bromophenyl)phenyl]sulfonylamino]-3-methylbutanoicaci;(S)-2-(4'-Bromo-[1,1'-biphenyl]-4-ylsulfonamido)-3-methylbutanoic acid
- 中文名:
- N-[(4'-溴[1,1'-联苯]-4-基)磺酰基]-L-缬氨酸
- 中文别名:
- 化合物 T20563;PD 166793,广谱MMP抑制剂;(S)-2-(4'-溴联苯-4-磺酰胺)-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-[1,1'-联苯]-4-基磺酰胺O)-3-甲基丁酸
- CBNumber:
- CB3840520
- 分子式:
- C17H18BrNO4S
- 分子量:
- 412.3
- MOL File:
- 199850-67-4.mol
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N-[(4'-溴[1,1'-联苯]-4-基)磺酰基]-L-缬氨酸化学性质
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熔点:
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192-193℃
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密度:
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1.457
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储存条件:
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Sealed in dry,2-8°C
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溶解度:
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DMF: 50 mg/ml; DMSO: 50 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: 10 mg/ml
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形态:
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A crystalline solid
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N-[(4'-溴[1,1'-联苯]-4-基)磺酰基]-L-缬氨酸性质、用途与生产工艺
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。
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MMP-2
4 nM (IC
50
)
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MMP-3
7 nM (IC
50
)
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MMP-13
8 nM (IC
50
)
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MMP-1
6.0 μM (IC
50
)
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MMP-7
7.2 μM (IC
50
)
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MMP-9
7.9 μM (IC
50
)
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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.
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Animal Model:
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Male Sprague-Dawley rats (6 weeks) were induced chronic biventricular volume overload
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Dosage:
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1 mg/kg
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Administration:
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Daily gavage beginning 2 weeks before surgery and continued until 8 weeks after surgery
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Result:
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Prevented ventricular dilatation and attenuated the hypertrophy typically induced by chronic volume overload.
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N-[(4'-溴[1,1'-联苯]-4-基)磺酰基]-L-缬氨酸
上下游产品信息
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下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | 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 |
| 2024/04/30 | HY-107428 | PD-166793 | | 10 mM * 1 mLin DMSO | 1210元 |
N-[(4'-溴[1,1'-联苯]-4-基)磺酰基]-L-缬氨酸
生产厂家
199850-67-4, N-[(4'-溴[1,1'-联苯]-4-基)磺酰基]-L-缬氨酸 相关搜索:
十溴联苯 2,2-联苯基-1-苦基肼基 6-(2,6-二氯苯基)-2-[[4-[2-(二乙基氨基)乙氧基]苯基]氨基]-8-甲基吡啶并[2,3-D]嘧啶-7(8H)-酮盐酸盐 6-(2,6-二氯苯基)-8-甲基-2-[[3-(甲硫基)苯基]氨基]吡啶并[2,3-D]嘧啶-7(8H)-酮 N-[(2R)-2,3-二羟基丙氧基]-3,4-二氟-2-[(2-氟-4-碘苯)氨基]苯甲酰胺 2-(2-氨基-3-甲氧基苯基)-4H-1-苯并吡喃-4-酮 2-[(2-氯-4-碘苯基)氨基]-N-(环丙基甲氧基)-3,4-二氟-苯甲酰胺 5-溴-N-(2,3-二羟基丙氧基)-3,4-二氟-2-[(2-氟-4-碘苯基)氨基]苯甲酰胺
- Protease inhibitor
- Angiogenesis and Metastasis
- 酶
- PD 166793,广谱MMP抑制剂
- 化合物 T20563
- (S)-2-(4'-溴联苯-4-磺酰胺)-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-[1,1'-联苯]-4-基磺酰胺O)-3-甲基丁酸
- 199850-67-4
- PD-166793-0000
- PD 166793 USP/EP/BP
- (2S)-2-[[4-(4-bromophenyl)phenyl]sulfonylamino]-3-methylbutanoicaci
- L-Valine, N-[(4'-bromo[1,1'-biphenyl]-4-yl)sulfonyl]-
- MMP-2/MMP-3 Inhibitor
- (S)-2-(4'-Bromo-[1,1'-biphenyl]-4-ylsulfonamido)-3-methylbutanoic acid
- N-[(4'-Bromo[1,1'-biphenyl]-4-yl)sulfonyl]-L-valine
- (S)-2-(4'-bromobiphenyl-4-ylsulfonamido)-3-methylbutanoic acid
- PD 166793