MK-886
MK-886 Basic information
- Product Name:
- MK-886
- Synonyms:
-
- L-663,536
- CS-1988
- 1-[(4-CHLOROPHENYL)METHYL]-3-[(1,1-DIMETHYLETHYL)THIO]-ALPHA,ALPHA-DIMETHYL-5-(1-METHYLETHYL)-1H-INDOLE-2-PROPANOIC ACID
- MK-886
- 3-[tert-Butylthio-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropionic Acid, Sodium Salt
- 3-[1-(4-Chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
- 3-[1-(4-Chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropionic acid
- 3-[3-tert-Butylthio-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropionic acid
- CAS:
- 118414-82-7
- MF:
- C27H34ClNO2S
- MW:
- 472.08
- Product Categories:
-
- All Inhibitors
- Inhibitors
- Prostanoid receptor and related
- Mol File:
- 118414-82-7.mol
MK-886 Chemical Properties
- Melting point:
- 295-297°C
- storage temp.
- Sealed in dry,2-8°C
- solubility
- DMSO: 32 mg/mL
- form
- White solid.
- color
- white
- Stability:
- Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months.
MK-886 Usage And Synthesis
Description
MK-886 (118414-82-7) is an inhibitor of leukotriene biosynthesis(IC50 = 2.5 nM in human PMN)1 via 5-lipoxygenase-activating protein (FLAP) inhibition (IC50 = 30 nM)2. MK-886 also inhibits PPARα (80% inhibition at 10 μM).3
Chemical Properties
White Solid
Uses
Binds to 5-lipoxygenase-activating protein with high affinity and prevents the activation of 5-lipoxygenase, thus inhibiting the biosynthesis of leukotrienes.
Uses
MK-886 is a potent and selective inhibitor of FLAP and Cox-1.
Definition
ChEBI: A member of the class of indoles that is 1H-indole substituted by a isopropyl group at position 5, a tert-butylsulfanediyl group at position 3, a 4-chlorobenzyl group at position 1 and a 2-carboxy-2-methylpropyl group at pos tion 2. It acts as an inhibitor of arachidonate 5-lipoxygenase.
Biological Activity
An inhibitor of leukotriene biosynthesis (IC 50 = 3 nM in human polymorphonuclear leukocytes). Acts by inhibiting 5-lipoxygenase-activating protein (FLAP) (IC 50 = 30 nM for inhibition of [ 125 I]-L-691,678 photoaffinity labelling). Also moderately potent PPAR α antagonist (IC 50 = 0.5-1 μ M). Orally active in vivo .
storage
Store at RT
References
References/Citations 1) Gillard et al (1989) 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; Can. .J. Physiol .Pharmacol. 67 456 2) Evans et al (1991) 5-Lipoxygenase-activating protein is the target of a quinoline class of leukotriene synthesis inhibitors; Mol. Pharmacol. 40 22 3) Kehrer et al (2001) Inhibition of peroxisome-proliferator-activated receptor (PPAR)α by MK886; Biochem. J. 356 899
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