GW311616,197890-44-1

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GW311616 hydrochloride

CAS No. : 197890-44-1

MCE 国际站：GW311616 hydrochloride

产品活性：GW-311616 是高活性，口服生物相容性，长效的人中性白细胞弹性蛋白酶 (HNE) 抑制剂，IC₅₀ 为 22 nM，K_i 为 0.31 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Elastase

In Vitro: GW-311616 (150 μM; 48 hours) markedly suppresses NE activity in U937 and K562 cells lines.
GW311616A (20-320 μM; 48 hours; U937 cells) treatment inhibits proliferation and induces apoptosis in leukemia cells.
GW-311616 (150 μM; U937 cells) treatment can increase the protein expression levels of Bax and decrease the expression of Bcl-2.

In Vivo: GW-311616 (2 mg/kg; oral administration) rapidly abolishes the circulation of neutrophil elastase (NE) in dogs, while >90% inhibition is maintained for 4 days. This prolonged effect is independent to be due to penetration of neutrophils in bone marrow by orally administrated GW-311616. GW-311616 has moderate terminal elimination half-life (t_1/2) of 1.1 hours and 1.5 hours for dog (2 mg/kg, oral), rat (2 mg/kg, oral), respectively.

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