Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PF-543 (Sphingosine Kinase 1 Inhibitor II) 是一种选择性可逆和鞘氨醇竞争性 SPHK1抑制剂,可诱导细胞凋亡、坏死和自噬。它对 SPHK1的选择性是 SPHK2 的 100 倍以上。它还抑制全血中 1-磷酸鞘氨醇形成,IC50为 26.7 nM。 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 PF-543 hydrochloride 的水溶性和稳定性通常比游离态更好。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 325 | 待询 | ||
5 mg | ¥ 717 | 待询 | ||
10 mg | ¥ 1,178 | 待询 | ||
25 mg | ¥ 1,750 | 待询 | ||
50 mg | ¥ 2,580 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 717 | 待询 |
PF-543 的其他形式现货产品:
产品描述 | PF-543 (Sphingosine Kinase 1 Inhibitor II), a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM. |
靶点活性 | SPHK1:3.6 nM(Ki), SPHK1:2.0 nM |
体外活性 | PF543 is a cell-permeable hydroxyl methylpyrrolidine compound that inhibits SphK-1/SphK1-catalyzed sphingosine phosphorylation in a reversible and sphingosine-competitive manner, exhibiting no affinity toward S1P receptors and much reduced inhibitory activity against Sphk2 (6.8% inhibition at 10 μM) or 46 other lipid and portein kinases (IC50 >10 μM). 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. PF-543 is 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. [1] |
体内活性 | Administration of the potent sphingosine kinase 1 inhibitor, PF-543 in a mouse hypoxic model of pulmonary hypertension has no effect on vascular remodelling but reduces right ventricular hypertrophy. Administration of 10 mg/kg PF-543 for 24 h to mice induces a decrease in SK1 expression in pulmonary vessels[2]. |
激酶实验 | FITC-S1P quantification/Caliper assay: A 384-well format of the SphK enzyme assay based on separation of FITC-S1P from unreacted FITC-sphingosine substrate using a microfluidic capillary electrophoresis mobility-shift system is developed. Briefly, 3 nM SphK1–His6 is incubated with 1 μM FITC-sphingosine, 20 μM ATP and 10 μM compound (a final concentration of DMSO of 2 %) in a buffer containing 100 mM Hepes (pH 7.4), 1 mM MgCl2,0.01% Triton X-100, 10% glycerol, 100 μM sodium orthovanadate and 1 mM DTT for 1 h in a 384-well Matrical MP-101-1-PP plate. Reaction mixtures (10 μL) are quenched by the addition of 20 μL of 30 mM EDTA and 0.15% Coating Reagent-3 in 100 mM Hepes, and a small aliquot of each reaction (a few nanolitres) is analysed in the Caliper LabChip 3000 instrument under -1.5 psi (psi=6.9 kPa) pressure, a downstream voltage of -1900 V and a sip time of 0.2 s. Phosphorylated fluorescent product and unphosphorylated fluorescent substrate appeared as distinctive peaks and are quantified using the Caliper data. |
细胞实验 | CellTiter-Glo Assay (Only for Reference) |
别名 | Sphingosine Kinase 1 Inhibitor II, PF 543 |
分子量 | 465.6 |
分子式 | C27H31NO4S |
CAS No. | 1415562-82-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: <1 mg/mL
DMSO: 93 mg/mL (199.74 mM)
Ethanol: 93 mg/mL (199.74 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.1478 mL | 10.7388 mL | 21.4777 mL | 53.6942 mL |
5 mM | 0.4296 mL | 2.1478 mL | 4.2955 mL | 10.7388 mL | |
10 mM | 0.2148 mL | 1.0739 mL | 2.1478 mL | 5.3694 mL | |
20 mM | 0.1074 mL | 0.5369 mL | 1.0739 mL | 2.6847 mL | |
50 mM | 0.043 mL | 0.2148 mL | 0.4296 mL | 1.0739 mL | |
100 mM | 0.0215 mL | 0.1074 mL | 0.2148 mL | 0.5369 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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