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MK-886

FLAP inhibitor
 
BML-EI266-0005 5 mg 86.00 USD
 
BML-EI266-0025 25 mg 344.00 USD
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Replaces Prod. #: ALX-270-368

Inhibitor of PPARα activation. Inhibits 5-lipoxygenase-activating protein (FLAP) and leukotriene biosynthesis. Binds to FLAP with high affinity and prevents the activation of 5-lipoxygenase. IC50’s for leukotriene biosynthesis: 2.5 nM in intact leukocytes; 1.1 µM in whole blood. Induces apoptosis through the mitochondrial pathway.

Product Specification

Alternative Name:L-663,536, 3-[1-(p-Chlorobenzyl)-5-(isopropyl)-3-t-butylthioindol-2-yl]-2,2-dimethylpropanoic acid . Na
 
Formula:C27H33ClNO2S·Na
 
MW:494.0
 
CAS:118414-82-7
 
Purity:≥98% (HPLC)
 
Appearance:White solid.
 
Solubility:Soluble in 100% ethanol (25mg/ml) or DMSO (25mg/ml).
 
Shipping:Ambient
 
Long Term Storage:Ambient
 
Use/Stability:Stable for at least 1 year after receipt when stored, as supplied, at room temperature. Prepare fresh solutions daily.
 
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Product Literature References

Mitochondria are direct targets of the lipoxygenase inhibitor MK886. A strategy for cell killing by combined treatment with MK886 and cyclooxygenase inhibitors: A. Gugliucci, et al.; J. Biol. Chem. 277, 31789 (2002), Abstract;
Inhibition of peroxisome-proliferator-activated receptor (PPAR)alpha by MK886: J.P. Kehrer, et al.; Biochem. J. 356, 899 (2001), Abstract;
FLAP: a novel drug target for inhibiting the synthesis of leukotrienes: A.W. Ford-Hutchinson; Trends Pharmacol. Sci. 12, 68 (1991), Abstract;
Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis: R.A. Dixon, et al.; Nature 343, 282 (1990), Abstract;
L-663,536 (MK-886) (3-[1-(4-chlorobenzyl)-3-t-butyl-thio-5-isopropylindol-2-yl]-2,2 - dimethylpropanoic acid), a novel, orally active leukotriene biosynthesis inhibitor: J. Gillard, et al.; Can. J. Physiol. Pharmacol. 67, 456 (1989), Abstract;

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