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Please store the product under the recommended conditions in the Certificate of Analysis.
- 英文名：
Sphingosine Kinase 1 Inhibitor II hydrochloride
- 库存：
货期：询盘
- 供应商：
MedChemExpress LLC
- CAS号：
1706522-79-3
- 规格：
询盘
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PF-543 hydrochloride
CAS No. : 1706522-79-3
MCE 国际站：PF-543 hydrochloride
产品活性：PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) 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 hydrochloride 对 SPHK1 的选择性是 SPHK2 的 100 倍以上。PF-543 hydrochloride 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 hydrochloride 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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文献和实验免疫荧光组织（细胞）化学技术系列七：现状与展望（附参考文献）
.（5）Akiyoshi Kawamura Jr. Fluorescent antibody Technique and Their Applications. Second Edition University of Tokyo Press, Tokyo, 1977; 79: P141~281.（6）蔡文琴, 王伯沄主编. 实用免疫细胞化学. 成都：四川科技出版社 1990，P968-977. （7）李成文. 现代免疫化学技术. 上海: 上海科技出版社 1992；P97-100. （8）Mahmudi
;96 (Nov):S707– 870. Practice Parameters for Allergy Diagnostic Testing. Ann Allergy Asthma Immunol 1995:75(Dec): 543–625. Practice Parameters for the Diagnosis and Management of Immunodeficiency. Ann Allergy Asthma Immunol 1996;76(March):282–294
托霉素：58%～76% 20mg/L胶原：47%～73% 78.血块收缩试验 定量法：48%～64% 试管法：1h开始收缩，24h完全收缩 血浆法：＞40% 79.血浆，-血小板球蛋白检测 -TG：（6.6～26.2）μg/L 80.血小板第4因子检测 PF4：（0.9～5.5）μg/L 81.P选择素检测 血浆P选择素（9.2～20.8）μg/L， 血小板P选择素数目（7900～10100）分子
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