475889
MK-886
≥99% (TLC), COX pathway blocker, solid
别名:
MK-886
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关于此项目
经验公式（希尔记法）:
C27H33ClNO2S · Na
化学文摘社编号:
分子量:
494.06
MDL number:
UNSPSC Code:
51111800
NACRES:
NA.77
产品名称
MK-886, A cell-permeable, orally active NSAID that blocks cellular Cox pathway PGE2 production by inhibiting COX-1 and mPGES-1, but not COX-2, activity, as well as suppresses cellular 5-LO pathway activation by inhibiting FLAP, rather than 5-LO, activity.
SMILES string
S(CCCC)c1c2c([n](c1CC(C)(C)C(=O)O)Cc3ccc(cc3)Cl)ccc(c2)C(C)C
InChI
1S/C27H34ClNO2S/c1-6-7-14-32-25-22-15-20(18(2)3)10-13-23(22)29(17-19-8-11-21(28)12-9-19)24(25)16-27(4,5)26(30)31/h8-13,15,18H,6-7,14,16-17H2,1-5H3,(H,30,31)
InChI key
VFMGWQLOCZBFCK-UHFFFAOYSA-N
assay
≥99% (TLC)
form
solid
potency
102 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
white
solubility
DMSO: 25 mg/mL
ethanol: 25 mg/mL
shipped in
ambient
storage temp.
10-30°C
Quality Level
Biochem/physiol Actions
产物不与ATP竞争。
可逆：否
细胞可渗透性：具有
主要靶标
白三烯生物合成
白三烯生物合成
Disclaimer
毒性：标准处理（A）
General description
一种可渗透细胞的口服活性NSAID（非甾体类抗炎药），可通过抑制COX-1和mPGES-1（微粒体PGE2合酶-1）而不是COX-2的活性（IC50分别为8、2和58 M）来阻断细胞Cox途径PGE2（前列腺素E2）的产生，并通过抑制FLAP（5-LO激活蛋白）而不是5-LO活性（1 M MK-886为<10%）来抑制细胞5-LO（5-脂氧合酶；目录号437996）途径的激活。与仅靶向COX途径的NSAID（非甾体类抗炎药）不同，MK-886在体内使用时不会引起胃肠道损害。
Other Notes
Koeberle, A., et al. 2009.Eur. J. Pharmacol.608, 84.
Koeberle, A., et al. 2008.J. Pharmacol.Exp.Ther.326, 975.
Fisher, L., et al. 2007.Br. J. Pharmacol.152, 471.
Ford-Hutchinson, A.W., et al. 1993.Can.J. Physiol.Pharmacol.71, 806.
Ford-Hutchinson, A.W.1991.Trends Pharmacol.12, 68.
Dixon, R.A., et al. 1990.Nature 343, 282.
Rouzer, C.A., et al. 1990.J. Biol. Chem.265, 1436.
Koeberle, A., et al. 2008.J. Pharmacol.Exp.Ther.326, 975.
Fisher, L., et al. 2007.Br. J. Pharmacol.152, 471.
Ford-Hutchinson, A.W., et al. 1993.Can.J. Physiol.Pharmacol.71, 806.
Ford-Hutchinson, A.W.1991.Trends Pharmacol.12, 68.
Dixon, R.A., et al. 1990.Nature 343, 282.
Rouzer, C.A., et al. 1990.J. Biol. Chem.265, 1436.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Ichitaro Abe et al.
Developmental cell, 57(23), 2623-2637 (2022-12-07)
De novo beige adipocyte biogenesis involves the proliferation of progenitor cells in white adipose tissue (WAT); however, what regulates this process remains unclear. Here, we report that in mouse models but also in human tissues, WAT lipolysis-derived linoleic acid triggers
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