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- 保存条件：
4°C, sealed storage, away from moisture
- 英文名：
Sphingosine Kinase 1 Inhibitor II Citrate
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1415562-83-2
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥693.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥280.0 |
| 规格： | 5 mg | 产品价格： | ￥630.0 |
| 规格： | 10 mg | 产品价格： | ￥1000.0 |
| 规格： | 50 mg | 产品价格： | ￥3200.0 |
| 规格： | 100 mg | 产品价格： | ￥4950.0 |
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PF-543 Citrate
CAS No. : 1415562-83-2
MCE 国际站：PF-543 Citrate
产品活性：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。
研究领域：Immunology/Inflammation | GPCR/G Protein | Apoptosis | Autophagy
作用靶点：SphK | LPL Receptor | Apoptosis | Autophagy
In Vitro: 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 C17-S1P formation in 1483 cells with an IC50 of 1.0 nM.
?SphK1 inhibition by PF-543 causes a dose-dependent depletion of the intracellular level of S1P with EC50 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.
In Vivo: 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 T1/2 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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文献和实验用量限制了这一治疗方案的广泛应用。目前诱导多能干细胞（iPSC）分化为产生胰岛素的 β 样细胞是一项重大进展。2021 年美国食品和药物管理局（FDA）已授予 VX-880（一种 iPSC 细胞在体外诱导分化而来的胰岛 β 细胞）快速通道指定，目前已启动 VX-880 的临床试验，用于治疗严重低血糖和低血糖意识受损的 1 型糖尿病（T1D）患者。在 2023 年 6 月举办的美国糖尿病协会 (ADA) 第 83 届科学会议上公布了正在进行的 VX-880 临床试验的积极结果：所有接受 VX-880 治疗的患者均
Metallomics Using Inductively Coupled Plasma Mass Spectrometry
proteins from a DEAE anion‐exchange column showing molybdenum (‐x‐) and protein (⋅⋅ o ⋅⋅) concentrations. Box shows fractions pooled for PF1972 purification (adapted from Cvetkovic et al., ). View Image
were significantly decreased. High expressions of Bcl-2 and Bax were detected in 1 and 2μmol/L arseni c trioxide-treated cells, these were 46%, 87.33% and 83.08%, 95.83% respecti vely, among which that of Bax was more significant. Arsenic trioxide treatment at 0.5μ
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