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CAS No.: 72873-74-6

SKF-86002 Catalog No. CSN13149

Synonyms: SKF-86002

SKF-86002 is a potent inhibitor of p38 MAP kinase with IC50 of 0.5-1 μM and inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50 = 1 μM).

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 p38 MAPK

IC50:0.5-1μM
描述SKF-86002 inhibited prostaglandin H2 (PGH2) synthase activity (IC₅₀ 120 μM) as well as prostanoid production in rat basophilic leukemia (RBL-1) cells (IC₅₀ 70 μM) and its sonicate (IC₅₀ 100 μM) and human monocytes (IC₅₀ 1 μM). In addition, SKF-86002 inhibited the generation of dihydroxyeicosatetraenoic acid (diHETE) and 5-hydroxyeicosatetraenoic acid (5-HETE) in a high speed supernatant fraction of RBL-1 cells (IC₅₀ 10 μM). Cellular production of 5-lipoxygenase products was inhibited by SKF-86002 as measured by leukotriene B4 (LTB4) generation from human neutrophils (IC₅₀ 20 μM), leukotriene C4 (LTC4) generation by human monocytes (IC₅₀ 20 μM), and 5-HETE production by RBL-1 cells (IC₅₀ 40 μM)^[3]. Apoptosis induced by stress stimuli activated p38 MAPK, and apoptosis was inhibited bySKF-86002^[4]. SKF-86002 blocked superoxide anion production in response to FMLP and reduced adhesion and chemotaxis in response to PAF or FMLP^[5]. In human osteoblastic cells (SaOS2) both basal and TNF alpha-stimulated IL6 production were inhibited in a concentration-related manner by SKF-86002but not by indomethacin^[6]. In vivo, profile of anti-inflammatory activity of SKF-86002 supports the dual inhibition of arachidonate metabolism as indicated by its activity in inflammation models that are insensitive to selective cyclooxygenase inhibitors. The responses of arachidonic-acid-induced edema in the mouse ear and rat paw, as well as the cell infiltration induced by carrageenan in the mouse peritoneum and by arachidonic acid in the rat air pouch, were inhibited by SKF-86002^[3].
动物研究
剂量
Mice: 5 mg/kg - 20 mg/kg^[3] (i.v.) Rat: 10 mg/kg^[4] (i.p.)

给药途径
i.v., i.p.
参考文献

动物研究
剂量	Mice: 5 mg/kg - 20 mg/kg^[3] (i.v.) Rat: 10 mg/kg^[4] (i.p.)
给药途径	i.v., i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.3630 mL
- 16.8152 mL
- 33.6304 mL
- 5 mM
- 0.6726 mL
- 3.3630 mL
- 6.7261 mL
- 10 mM
- 0.3363 mL
- 1.6815 mL
- 3.3630 mL

技术信息

CAS号

72873-74-6

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H12FN3S

运输

蓝冰

分子量

297.35

别名

SKF-86002

溶解度

DMSO	30.0 mg/mL (100.9 mM) warming

动物实验配方

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SKF-86002 Catalog No. CSN13149

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