CS-1261
| 中文名称 | CS-1261 |
|---|---|
| 中文同义词 | 化合物 T11525 |
| 英文名称 | (3S,3AS,6AR)-3-ISOPROPYL-1-(METHANESULFONYL)-4-[4-(1-PIPERIDINYL)-2(E)-BUTENOYL]PERHYDROPYRROLO[3,2B]PYRROL-2(1H)-ONE HYDROCHLORIDE |
| 英文同义词 | (3S,3AS,6AR)-3-ISOPROPYL-1-(METHANESULFONYL)-4-[4-(1-PIPERIDINYL)-2(E)-BUTENOYL]PERHYDROPYRROLO[3,2B]PYRROL-2(1H)-ONE HYDROCHLORIDE;(3S,3AS,6AR)-HEXAHYDRO-3-(1-METHYLETHYL)-1-(METHYLSULFONYL)-4-[(2E)-1-OXO-4-(1-PIPERIDINYL)-2-BUTENYL]PYRROLO[3,2-B]PYRROL-2(1H)-ONE HYDROCHLORIDE;GW311616A;GW 311616 HYDROCHLORIDE;(3S,3aS,6aR)-Hexahydro-3-(1-methylethyl)-1-(methylsulfonyl)-4-((2E)-1-oxo-4-(1-piperidinyl)-2-butenyl)pyrrolo[3.2-b]pyrr;GW311616HCl;GW311616;CS-1261 |
| CAS号 | 198062-54-3 |
| 分子式 | C19H31N3O4S |
| 分子量 | 397.53 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 198062-54-3.mol |
| 结构式 |  |
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) |
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. |
| 提供商 | 语言 |
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英文
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| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-15891 | CS-1261 GW311616 | 198062-54-3 | 2mg | 2190元 |
| 2024/04/30 | HY-15891 | CS-1261 GW311616 | 198062-54-3 | 5mg | 3510元 |