SSR69071,344930-95-6

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SSR69071

CAS No. : 344930-95-6

MCE 国际站：SSR69071

产品活性：SSR69071 是一种有效的，具有口服活性的选择性中性粒细胞弹性蛋白酶 (neutrophil elastase) 抑制剂。SSR69071 减少缺血再灌注损伤后的心肌梗死面积。SSR69071 对人弹性蛋白酶 (K_i=0.0168 nM) 的亲和力高于对大鼠 (K_i=3 nM)、小鼠 (K_i=1.8 nM) 和兔 (K_i=58 nM) 弹性蛋白酶。

研究领域：Metabolic Enzyme/Protease

作用靶点：Elastase

In Vitro: SSR69071 is a potent inhibitor of human leukocyte elastase (HLE), with the inhibition constant (K_i) and the constant for inactivation process (k_on) being 0.0168±0.0014 nM and 0.183±0.013 10⁶/mol sr, respectively.
SSR69071 is a potent, competitive and slow tight binding inhibitor of HLE in vitro with a K_i value of 16.8 pM.

In Vivo: SSR69071 (3 mg/kg i.v.) reduces cardiac infarct size when administered before ischemia or just prior to reperfusion.

Treatment with SSR69071 (3 mg/kg i.v.) just prior to reperfusion significantly reduces cardiac elastase activity.
Bronchoalveolar lavage fluid from mice orally treated with SSR69071 inhibits HLE (ex vivo), and in this model, SSR69071 has a dose-dependent efficacy with an ED₅₀=10.5 mg/kg p.o. SSR69071 decreases significantly the acute lung hemorrhage induced by HLE (ED₅₀=2.8 mg/kg p.o.) in mice. SSR69071 prevents carrageenan- (ED₃₀=2.2 mg/kg) and HLE-induced (ED₃₀=2.7 mg/kg) paw edema in rats after p.o. administration.

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