CS-1261
CS-1261 性质
| 沸点 | 583.6±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.27±0.1 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | H2O：24 mg/mL，可溶 |
| 形态 | 固体 |
| 酸度系数(pKa) | 8.53±0.10(Predicted) |
| 颜色 | 浅棕色至棕色 |
CS-1261 用途与合成方法
IC50: 22 nM (HNE) Ki: 0.31 nM (HNE)
GW-311616 (150 μM; 48 hours) markedly suppresses NE activity in U937 and K562 cells lines.
GW-311616 (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
| 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
| 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. |
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 was achieved 6 hours after dosing, with activity returning towards control values. Single oral dose of 2 mg/kg rapidly abolished circulating enzyme activity, and greater than 90% inhibition was maintained for 4 days. |
CS-1261 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-11-08 | HY-15891A | 1 mg | 1840 | ||
| 2024-11-08 | HY-15891 | CS-1261 | 198062-54-3 | 2mg | 2190 |
