From Wikipedia, the free encyclopedia
MK-886
Names
Preferred IUPAC name
3-{3-(tert -Butylsulfanyl)-1-[(4-chlorophenyl)methyl]-5-(propan-2-yl)-1H -indol-2-yl}-2,2-dimethylpropanoic acid
Other names
L-663536
Identifiers
MeSH
L+663536
UNII
CC(C)C1=CC2=C(C=C1)N(C(=C2SC(C)(C)C)CC(C)(C)C(=O)O)CC3=CC=C(C=C3)Cl
Properties
C27 H34 ClNO2 S
Molar mass
472.083
Except where otherwise noted, data are given for materials in their
standard state (at 25 °C [77 °F], 100 kPa).
Chemical compound
MK-886 , or L-663536 , is a
leukotriene antagonist . It may perform this by blocking the
5-lipoxygenase activating protein (FLAP), thus inhibiting
5-lipoxygenase (5-LOX),
[1] and may help in treating
atherosclerosis .
[2]
References
^ Jun, Joon-Il; Lau, Lester F. (July 2010).
"The matricellular protein CCN1 induces fibroblast senescence and restricts fibrosis in cutaneous wound healing" . Nature Cell Biology . 12 (7): 676–685.
doi :
10.1038/ncb2070 .
ISSN
1465-7392 .
PMC
2919364 .
PMID
20526329 .
^ Jawien, J.; Gajda, M.; Rudling, M.; Mateuszuk, L.; Olszanecki, R.; Guzik, T. J.; Cichocki, T.; Chlopicki, S.; Korbut, R. (March 2006). "Inhibition of five lipoxygenase activating protein (FLAP) by MK-886 decreases atherosclerosis in apoE/LDLR-double knockout mice". European Journal of Clinical Investigation . 36 (3): 141–146.
doi :
10.1111/j.1365-2362.2006.01606.x .
PMID
16506957 .
S2CID
44897529 .
Receptor (
ligands )
BLT Tooltip Leukotriene B4 receptor
BLT1 Tooltip Leukotriene B4 receptor 1
BLT2 Tooltip Leukotriene B4 receptor 2
CysLT Tooltip Cysteinyl leukotriene receptor
CysLT1 Tooltip Cysteinyl leukotriene receptor 1
CysLT2 Tooltip Cysteinyl leukotriene receptor 2
CysLTE Tooltip Cysteinyl leukotriene receptor E
Enzyme (
inhibitors )
5-LOX Tooltip Arachidonate 5-lipoxygenase
12-LOX Tooltip Arachidonate 12-lipoxygenase
15-LOX Tooltip Arachidonate 15-lipoxygenase
LTA4 H Tooltip Leukotriene A4 hydrolase
LTB4 H Tooltip Leukotriene B4 ω-hydroxylase
LTC4 S Tooltip Leukotriene C4 synthase
LTC4 H Tooltip Leukotriene C4 hydrolase
LTD4 Tooltip Leukotriene D4 hydrolase
Others
PPARα Tooltip Peroxisome proliferator-activated receptor alpha
PPARδ Tooltip Peroxisome proliferator-activated receptor delta
PPARγ Tooltip Peroxisome proliferator-activated receptor gamma Non-selective