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PF-543 HCl

目录号 M10599 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


PF-543 HCl 是一种有效的,选择性的,可逆和鞘氨醇竞争性的 SPHK1 抑制剂,IC50 为 2 nM,Ki 为 3.6 nM。PF-543 hydrochloride 对 SPHK1 的选择性是 SPHK2 的 100 倍以上。PF-543 HCl可诱导细胞凋亡、坏死和自噬。

PF-543 HCl结构式

别名:PF-543 HCl; PF543 hydrochloride

规格 价格 库存状态
5mg ¥ 810 中国库存现货
10mg ¥ 1215 中国库存现货
其他规格数量报价?

质量标准及产品资料
生物活性

PF-543 hydrochloride is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 was effective as a potent inhibitor of S1P formation in whole blood, indicating that the SphK1 isoform of sphingosine kinase is the major source of S1P in human blood. In the SphK1-overexpression 1483 head and neck carcinoma cells, PF-543 decreases the level of endogenous S1P 10-fold with a proportional increase in the level of sphingosine. PF-543 binds SphK1 reversibly (k off t1/2=8.5 min) and with high affinity and the binding constant (Kd) is 5 nM. PF543 had no effect on the proliferation and survival of 1483, A549, LN229, Jurkat, U937 and MCF-7 cells, despite a dramatic change in the cellular S1P/sphingosine ratio. 

In vivo, administration of 10 mg/kg PF-543 for 24 h to mice induces a decrease in SK1 expression in pulmonary vessels.

实验参考
体外实验*
细胞系 1483, A549, LN229, Jurkat, U937, MCF-7
方法 1483 cells were cultured in DMEM/Ham’s F-12, A549 and LN229 cells were cultured in DMEM, Jurkat and U937 cells were cultured in RPMI 1640, and MCF-7 cells were cultured in Eagle’s MEM (minimal essential medium) with 0.01 mg/ml insulin. All media were supplemented with L-glutamine, Gentamicin and 10% FBS (or 0.5% FBS as indicated). The cells were grown in 96-well plates in 100 μl of medium with PF-543 or DMSO vehicle (0.01%) at 37 ◦C in an humidified incubator in the presence of 5% CO2. The cell growth and viability was measured using the CellTiter-Glo® Assay (Promega) by quantifying luminescence proportional to the amount of ATP present according to the manufacturer’s protocol.
浓度 ~1 μM
处理时间 7 days

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

体内实验*
动物模型 Female C57BL/6 J mice (7-12 week-old) with hypoxic-induced pulmonary arterial hypertension
配制 dissolved in vehicle (20% (2-Hydroxypropyl)-β-cyclodextrin in phosphate buffered saline (PBS))
剂量 1 mg/kg
给药处理 Intraperitoneal injection; every second day; for 21 days

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

化学性质
分子量 502.07
分子式 C27H32ClNO4S
CAS号 1706522-79-3
溶解性(25°C) DMSO ≥ 60 mg/mL
储存条件 粉末型式       -20°C   3年;4°C   2年
溶于溶剂       -80°C   6个月;-20°C   1个月
运输方式 冰袋运输,根据产品的不同,可能会有相应调整。
储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.9918 mL 9.9588 mL 19.9175 mL
5 mM 0.3984 mL 1.9918 mL 3.9835 mL
10 mM 0.1992 mL 0.9959 mL 1.9918 mL
不同实验动物依据体表面积的等效剂量转换表(参考来源于公开文献
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Masakazu Hamada, et al. Cell Death Discov. Induction of autophagy by sphingosine kinase 1 inhibitor PF-543 in head and neck squamous cell carcinoma cells

[2] Neil MacRitchie, et al. Cell Signal. Effect of the sphingosine kinase 1 selective inhibitor, PF-543 on arterial and cardiac remodelling in a hypoxic model of pulmonary arterial hypertension

[3] Mark E Schnute, et al. Biochem J. Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1

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