网站主页 >> CAS数据库列表 >> (2R)-1-[[4-[[3-甲基-5-[(苯磺酰基)甲基]苯氧基]甲基]苯基]甲基]-2-吡咯烷甲醇柠檬酸盐
(2R)-1-[[4-[[3-甲基-5-[(苯磺酰基)甲基]苯氧基]甲基]苯基]甲基]-2-吡咯烷甲醇柠檬酸盐
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- CAS号:
- 1415562-83-2
- 英文名:
- PF-543 (Citrate)
- 英文别名:
- PF-543 (Citrate);PWXXWUWKNPXSGW-VQIWEWKSSA-N;PF543 CITRATE; PF 543 CITRATE;Sphingosine Kinase 1 Inhibitor II Citrate;(2R)-1-[[4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol 2-hydroxy-1,2,3-propanetricarboxylate;(2R)-1-[[4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
- 中文名:
- (2R)-1-[[4-[[3-甲基-5-[(苯磺酰基)甲基]苯氧基]甲基]苯基]甲基]-2-吡咯烷甲醇柠檬酸盐
- 中文别名:
- 化合物 T12436;SPHK1抑制剂(PF-543 CITRATE);(2R)-1-[[4-[[3-甲基-5-[(苯磺酰基)甲基]苯氧基]甲基]苯基]甲基]-2-吡咯烷甲醇柠檬酸盐
- CBNumber:
- CB12645149
- 分子式:
- C33H39NO11S
- 分子量:
- 657.73
- MOL File:
- 1415562-83-2.mol
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(2R)-1-[[4-[[3-甲基-5-[(苯磺酰基)甲基]苯氧基]甲基]苯基]甲基]-2-吡咯烷甲醇柠檬酸盐化学性质
(2R)-1-[[4-[[3-甲基-5-[(苯磺酰基)甲基]苯氧基]甲基]苯基]甲基]-2-吡咯烷甲醇柠檬酸盐性质、用途与生产工艺
PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) 是一种有效，选择性，可逆和鞘氨醇竞争性 SPHK1 抑制剂，IC50 为 2 nM，Ki 为 3.6 nM。PF-543 Citrate 对 SPHK1 的选择性是 SPHK2 的 100 倍以上。PF-543 Citrate 还是有效的全血中 1-磷酸鞘氨醇 (S1P) 形成的有效抑制剂，IC50 为 26.7 nM。PF-543 Citrate 诱导细胞凋亡，坏死和自噬。
IC50: 2 nM (SPHK1); 26.7 nM (Sphingosine 1-phosphate (S1P))
Ki: 3.6 nM (SPHK1)
PF-543 (10-1000 nM; 24 hours; PASM cells) treatment abolishes SK1 expression at nM concentrations.
PF-543 (0.1-10 μM; 24 hours; PASM cells) treatment induces caspase-3/7 activity.
PF-543 inhibits C
17
-S1P formation in 1483 cells with an IC
50
of 1.0 nM.
SphK1 inhibition by PF-543 causes a dose-dependent depletion of the intracellular level of S1P with EC
50
concentration of 8.4 nM and a concomitant elevation of the intracellular level of sphingosine in 1483 cells. The level of endogenous S1P in 1483 cells after a 1 h treatment with 200 nM PF-543 is decreased 10-fold, producing a proportional increase in the level of sphingosine.
Western Blot Analysis
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Cell Line:
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Human pulmonary arterial smooth muscle (PASM) cells
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Concentration:
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10 nM, 100 nM, 1000 nM
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Incubation Time:
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24 hours
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Result:
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Abolished SK1 expression at nM concentrations.
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Apoptosis Analysis
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Cell Line:
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Human pulmonary arterial smooth muscle (PASM) cells
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Concentration:
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0.1 μM, 1 μM, 10 μM
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Incubation Time:
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24 hours
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Result:
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Induced caspase-3/7 activity in cultured human pulmonary smooth muscle cells.
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PF-543 (1 mg/kg; intraperitoneal injection; every second day; for 21 days; female C57BL/6 J mice) treatment has no effect on vascular remodelling but reduces right ventricular hypertrophy. The protection involves a reduction in the expression of p53 and an increase in the expression of anti-oxidant nuclear factor Nrf-2.
Mice are initially dosed (ip) with 10 mg/kg or 30 mg/kg of PF-543 for 24 h and the T
1/2
is 1.2 h in blood samples. Administration of 10 mg/kg PF-543 for 24 h to mice induces a decrease in SK1 expression in pulmonary vessels.
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Animal Model:
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Female C57BL/6 J mice (7-12 week-old) with hypoxic-induced pulmonary arterial hypertension
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Dosage:
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1 mg/kg
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Administration:
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Intraperitoneal injection; every second day; for 21 days
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Result:
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Reduced right ventricular hypertrophy. The protection involves a reduction in the expression of p53 (that promotes cardiomyocyte death) and an increase in the expression of anti-oxidant nuclear factor Nrf-2.
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(2R)-1-[[4-[[3-甲基-5-[(苯磺酰基)甲基]苯氧基]甲基]苯基]甲基]-2-吡咯烷甲醇柠檬酸盐
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 |
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| 2024/01/25 | HY-15425A | PF-543 Citrate | | 1 mg | 340元 |
| 2024/01/25 | HY-15425A | (2R)-1-[[4-[[3-甲基-5-[(苯磺酰基)甲基]苯氧基]甲基]苯基]甲基]-2-吡咯烷甲醇柠檬酸盐
PF-543 Citrate | 1415562-83-2 | 5mg | 750元 |
(2R)-1-[[4-[[3-甲基-5-[(苯磺酰基)甲基]苯氧基]甲基]苯基]甲基]-2-吡咯烷甲醇柠檬酸盐
生产厂家
1415562-83-2, (2R)-1-[[4-[[3-甲基-5-[(苯磺酰基)甲基]苯氧基]甲基]苯基]甲基]-2-吡咯烷甲醇柠檬酸盐 相关搜索:
- 细胞生物学试剂
- C6H8O7C27H31NO4S
- C33H39NO11S
- C27H31NO4SC6H8O7
- 化合物 T12436
- SPHK1抑制剂(PF-543 CITRATE)
- (2R)-1-[[4-[[3-甲基-5-[(苯磺酰基)甲基]苯氧基]甲基]苯基]甲基]-2-吡咯烷甲醇柠檬酸盐
- 1415562-83-2
- Sphingosine Kinase 1 Inhibitor II Citrate
- PF543 CITRATE; PF 543 CITRATE
- PWXXWUWKNPXSGW-VQIWEWKSSA-N
- (2R)-1-[[4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol 2-hydroxy-1,2,3-propanetricarboxylate
- (2R)-1-[[4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
- PF-543 (Citrate)