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BAY-85-8501

CAS No. : 1161921-82-9

MCE 站：BAY-85-8501

产品活性：BAY-85-8501 是人类中性脂酶 (HNE) 的一个有效的、选择性抑制剂，其 IC₅₀ 值为 65 pM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Elastase

In Vivo: In this model the exogenous HNE noxa is the primary cause of injury ａnd lung hemorrhage. Based on picomolar potency against HNE as well as single digit potency versus MNE, BAY-85-8501 (29) completely prevents the development of lung injury ａnd subsequent inflammation when administered 1 h prior to the HNE noxa. In the 0.01 mg/kg dose group, hemoglobin concentration is already significantly decreased. At a dose of 0.1 mg/kg, a significant effect on neutrophil ｃount is observed. In this setup, efficacy is predominantly driven by potency against HNE (K_i=0.08 nM). As the highly HNE-selective inhibitor BAY 85-8501 has no effect on PPE, BAY-85-8501 could not prevent the primary lung injury in this setup. Nevertheless, BAY-85-8501 could inhibit MNE, the endogenous driver of inflammation ａnd secondary injury, although with decreased potency. Consequently, the effects of BAY-85-8501 on inflammation ａnd secondary injury are weaker at this point, ａnd only observed at 30-fold higher doses. Efficacy is predominantly driven by potency against MNE (K_i=6 nM) in this second setup.

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