SKF-86002

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Chemical Structure| 72873-74-6 同义名 : -
CAS号 : 72873-74-6
货号 : A251928
分子式 : C16H12FN3S
纯度 : 99%+
分子量 : 297.35
MDL号 : MFCD00869367
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.36mL

0.67mL

0.34mL

16.82mL

3.36mL

1.68mL

33.63mL

6.73mL

3.36mL
参考文献

[1]Frasch SC, Nick JA, et al. p38 mitogen-activated protein kinase-dependent and -independent intracellular signal transduction pathways leading to apoptosis in human neutrophils. J Biol Chem. 1998 Apr 3;273(14):8389-97.

[2]Griswold DE, Marshall PJ, et al. SK&F 86002: a structurally novel anti-inflammatory agent that inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid. Biochem Pharmacol. 1987 Oct 15;36(20):3463-70.

[3]Griswold DE, Marshall PJ, Webb EF, Godfrey R, Newton J Jr, DiMartino MJ, Sarau HM, Gleason JG, Poste G, Hanna N. SK&F 86002: a structurally novel anti-inflammatory agent that inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid. Biochem Pharmacol. 1987 Oct 15;36(20):3463-70. doi: 10.1016/0006-2952(87)90327-3. PMID: 2823821.

[4]Frasch SC, Nick JA, Fadok VA, Bratton DL, Worthen GS, Henson PM. p38 mitogen-activated protein kinase-dependent and -independent intracellular signal transduction pathways leading to apoptosis in human neutrophils. J Biol Chem. 1998 Apr 3;273(14):8389-97. doi: 10.1074/jbc.273.14.8389. PMID: 9525949.

[5]Nick JA, Avdi NJ, Young SK, Knall C, Gerwins P, Johnson GL, Worthen GS. Common and distinct intracellular signaling pathways in human neutrophils utilized by platelet activating factor and FMLP. J Clin Invest. 1997 Mar 1;99(5):975-86. doi: 10.1172/JCI119263. PMID: 9062356; PMCID: PMC507906.

[6]Blanque R, Cottereaux C, Gardner CR. Effects of SK&F 86002 on cytokine-stimulated IL6 production in cultured neonatal mouse calvaria and SaOS2 osteoblastic cells: the role of prostaglandins and other mechanisms of action. Drugs Exp Clin Res. 1997;23(2):63-70. PMID: 9309381.