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1415562-83-2

中文名稱 (2R)-1-[[4-[[3-甲基-5-[(苯磺?;?甲基]苯氧基]甲基]苯基]甲基]-2-吡咯烷甲醇檸檬酸鹽
英文名稱 PF-543 (Citrate)
CAS 1415562-83-2
分子式 C33H39NO11S
分子量 657.728
MOL 文件 1415562-83-2.mol
更新日期 2024/11/15 18:20:33
1415562-83-2 結(jié)構(gòu)式 1415562-83-2 結(jié)構(gòu)式

基本信息

中文別名
SPHK1抑制劑(PF-543 CITRATE)
(2R)-1-[[4-[[3-甲基-5-[(苯磺?;?甲基]苯氧基]甲基]苯基]甲基]-2-吡咯烷甲醇檸檬酸鹽
英文別名
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)
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

形態(tài)Powder
顏色White to yellow

常見問題列表

生物活性
PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) 是一種有效,選擇性,可逆和鞘氨醇競爭性 SPHK1 抑制劑,IC50 為 2 nM,Ki 為 3.6 nM。PF-543 Citrate 對 SPHK1 的選擇性是 SPHK2 的 100 倍以上。PF-543 Citrate 還是有效的全血中 1-磷酸鞘氨醇 (S1P) 形成的有效抑制劑,IC50 為 26.7 nM。PF-543 Citrate 誘導(dǎo)細胞凋亡,壞死和自噬。
靶點

IC50: 2 nM (SPHK1); 26.7 nM (Sphingosine 1-phosphate (S1P))
Ki: 3.6 nM (SPHK1)

體外研究

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

Cell Line: Human pulmonary arterial smooth muscle (PASM) cells
Concentration: 10 nM, 100 nM, 1000 nM
Incubation Time: 24 ?hours
Result: Abolished SK1 expression at nM concentrations.

Apoptosis Analysis

Cell Line: Human pulmonary arterial smooth muscle (PASM) cells
Concentration: 0.1 μM, 1 μM, 10 μM
Incubation Time: 24 ?hours
Result: Induced caspase-3/7 activity in cultured human pulmonary smooth muscle cells.
體內(nèi)研究

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.

Animal Model: Female C57BL/6 J mice (7-12 week-old) with hypoxic-induced pulmonary arterial hypertension
Dosage: 1 mg/kg
Administration: Intraperitoneal injection; every second day; for 21 days
Result: 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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