CS-1261
|
|
|
- CAS号:
- 198062-54-3
- 英文名:
- (3S,3AS,6AR)-3-ISOPROPYL-1-(METHANESULFONYL)-4-[4-(1-PIPERIDINYL)-2(E)-BUTENOYL]PERHYDROPYRROLO[3,2B]PYRROL-2(1H)-ONE HYDROCHLORIDE
- 英文别名:
- CS-1261;GW311616;GW311616A;GW311616HCl;GW311616,GW-311616;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;(3S,3AS,6AR)-3-ISOPROPYL-1-(METHANESULFONYL)-4-[4-(1-PIPERIDINYL)-2(E)-BUTENOYL]PERHYDROPYRROLO[3,2B]PYRROL-2(1H)-ONE HYDROCHLORIDE;Pyrrolo[3,2-b]pyrrol-2(1H)-one, hexahydro-3-(1-methylethyl)-1-(methylsulfonyl)-4-[(2E)-1-oxo-4-(1-piperidinyl)-2-buten-1-yl]-, (3S,3aS,6aR)-;(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
- 中文名:
- CS-1261
- 中文别名:
- 化合物 T11525
- CBNumber:
- CB2420576
- 分子式:
- C19H31N3O4S
- 分子量:
- 397.53
- MOL File:
- 198062-54-3.mol
|
|
|
CS-1261化学性质
-
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, soluble
-
|
-
形态:
-
solid
-
|
-
酸度系数(pKa):
-
8.53±0.10(Predicted)
-
|
-
颜色:
-
Light brown to brown
-
|
CS-1261性质、用途与生产工艺
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，Ki 为 0.31 nM。
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
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
198062-54-3, CS-1261 相关搜索:
- C19H31N3O4S
- 化合物 T11525
- 198062-54-3
- GW311616,GW-311616
- Pyrrolo[3,2-b]pyrrol-2(1H)-one, hexahydro-3-(1-methylethyl)-1-(methylsulfonyl)-4-[(2E)-1-oxo-4-(1-piperidinyl)-2-buten-1-yl]-, (3S,3aS,6aR)-
- CS-1261
- GW311616
- GW311616HCl
- (3S,3aS,6aR)-Hexahydro-3-(1-methylethyl)-1-(methylsulfonyl)-4-((2E)-1-oxo-4-(1-piperidinyl)-2-butenyl)pyrrolo[3.2-b]pyrr
- GW 311616 HYDROCHLORIDE
- GW311616A
- (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
- (3S,3AS,6AR)-3-ISOPROPYL-1-(METHANESULFONYL)-4-[4-(1-PIPERIDINYL)-2(E)-BUTENOYL]PERHYDROPYRROLO[3,2B]PYRROL-2(1H)-ONE HYDROCHLORIDE