CS-1260
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- CAS號(hào):
- 197890-44-1
- 英文名:
- GW311616A
- 英文別名:
- CS-1260;GW 311616A;GW-311616A;GW 311616A - GW 311616 hydrochloride;GW311616 hydrochloride,GW-311616 hydrochloride
- 中文名:
- CS-1260
- 中文別名:
- 化合物 T11525L;化合物 GW311616 HYDROCHLORIDE
- CBNumber:
- CB8498151
- 分子式:
- C19H32ClN3O4S
- 分子量:
- 433.99
- MOL File:
- 197890-44-1.mol
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CS-1260化學(xué)性質(zhì)
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儲(chǔ)存條件:
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2-8°C
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溶解度:
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H2O: 24 mg/mL, soluble
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形態(tài):
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solid
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顏色:
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White to yellow
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CS-1260性質(zhì)、用途與生產(chǎn)工藝
GW-311616 是高活性，口服生物相容性，長(zhǎng)效的人中性白細(xì)胞彈性蛋白酶 (HNE) 抑制劑，IC50 為 22 nM，Ki 為 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.
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
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Cell Line:
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U937 and K562 cells
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Concentration:
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150 μM
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Incubation Time:
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48 hours
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Result:
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Markedly suppressed NE activity.
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Apoptosis Analysis
[2]
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Cell Line:
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U937 cells
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Concentration:
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20 μM, 40 μM, 80 μM, 160 μM, 320 μM
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Incubation Time:
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48 hours
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Result:
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The rate of apoptosis was enhanced.
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Western Blot Analysis
[2]
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Cell Line:
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U937 cells
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Concentration:
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150 μM
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Incubation Time:
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48 hours
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Result:
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Increased the protein expression levels of Bax and decreased the expression of Bcl-2.
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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.
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Animal Model:
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Dogs (9-month-old)
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Dosage:
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0.22 mg/kg, 0.66 mg/kg and 2 mg/kg (Pharmacokinetic study)
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Administration:
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Oral administration
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Result:
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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.
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CS-1260
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
197890-44-1, CS-1260 相關(guān)搜索:
- 抑制劑
- 化合物 GW311616 HYDROCHLORIDE
- 化合物 T11525L
- 197890-44-1
- GW311616 hydrochloride,GW-311616 hydrochloride
- GW 311616A - GW 311616 hydrochloride
- GW 311616A;GW-311616A
- CS-1260