199850-67-4

中文名称 N-[(4'-溴[1,1'-联苯]-4-基)磺酰基]-L-缬氨酸

英文名称 PD 166793

CAS 199850-67-4

分子式 C17H18BrNO4S

分子量 412.3

MOL 文件 199850-67-4.mol

199850-67-4 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

(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

英文别名

PD 166793
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

所属类别

生物化工：缬氨酸类衍生物

物理化学性质

熔点192-193℃

密度1.457

储存条件Sealed in dry,2-8°C

溶解度DMF: 50 mg/ml; DMSO: 50 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: 10 mg/ml

形态结晶固体

颜色White to pink

常见问题列表

生物活性

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。

靶点

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 )

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.

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 (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.