中文名 | GW311616 (hydrochloride) |
英文名 | GW311616 (hydrochloride) |
别名 | 化合物 T11525L |
英文别名 | CS-1260 GW311616A GW 311616A GW-311616A GW311616 (hydrochloride) GW 311616A - GW 311616 hydrochloride |
CAS | 197890-44-1 |
化学式 | C19H32ClN3O4S |
分子量 | 433.99 |
溶解度 | H2O: 24mg/ml,可溶 |
存储条件 | 2-8°C |
外观 | 固体 |
体外研究 | 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. Cell Viability Assay Cell Line: U937 and K562 cells Concentration: 150 μM Incubation Time: 48 hours Result: Markedly suppressed NE activity. Apoptosis Analysis [2] Cell Line: U937 cells Concentration: 20 μM, 40 μM, 80 μM, 160 μM, 320 μM Incubation Time: 48 hours Result: The rate of apoptosis was enhanced. Western Blot Analysis [2] Cell Line: U937 cells Concentration: 150 μM Incubation Time: 48 hours Result: Increased the protein expression levels of Bax and decreased the expression of Bcl-2. |
体内研究 | 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. Animal Model: Dogs (9-month-old) Dosage: 0.22 mg/kg, 0.66 mg/kg and 2 mg/kg (Pharmacokinetic study) Administration: Oral administration Result: At 0.22 mg/kg, greater than 50% inhibition of elastase is achieved 6 hours after dosing, with activity returning towards control values. Single oral dose of 2 mg/kg rapidly abolishes circulating enzyme activity, and greater than 90% inhibition is maintained for 4 days. |
危险品标志 | Xi - 刺激性物品 |
风险术语 | 36/37/38 - 刺激眼睛、呼吸系统和皮肤。 |
安全术语 | S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S36 - 穿戴适当的防护服。 |
WGK Germany | 3 |
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