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
- 中文名:CS-1261
- CBNumber:CB2420576
- 分子式:C19H31N3O4S
- 分子量:397.53
- MOL File:198062-54-3.mol
- 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
- 生物活性 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，Ki 为 0.31 nM。
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靶点
IC50: 22 nM (HNE) Ki: 0.31 nM (HNE)
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体外研究
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. -
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 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.
- 更新日期：2024/11/08
- 产品编号：HY-15891A
- 产品名称：GW311616 hydrochloride
- CAS编号：
- 包装：1 mg
- 价格：1840元
- 更新日期：2024/11/08
- 产品编号：HY-15891
- 产品名称：CS-1261 GW311616
- CAS编号：198062-54-3
- 包装：2mg
- 价格：2190元
- 公司名称：SIGMA
- 联系电话：--
- 电子邮件：
- 国家：瑞士
- 产品数：6896
- 优势度：91
