199850-67-4
199850-67-4 結(jié)構(gòu)式
基本信息
N-[(4'-溴[1,1'-聯(lián)苯]-4-基)磺?；鵠-L-纈氨酸
(S)-2-(4'-溴-[1,1'-聯(lián)苯]-4-基磺酰胺O)-3-甲基丁酸
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
物理化學(xué)性質(zhì)
常見問題列表
|
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. |