MK-886
Synonym(s):3-[1-( p-Chlorobenzyl)-5-(isopropyl)-3- t-butylthioindol-2-yl]-2,2-dimethylpropanoic Acid, Na, COX-1 Inhibitor III, FLAP Inhibitor I, MK886, mPGES-1 Inhibitor I;MK-886 - CAS 118414-82-7 - Calbiochem
- CAS NO.:118414-82-7
- Empirical Formula: C27H34ClNO2S
- Molecular Weight: 472.08
- MDL number: MFCD00876710
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is MK-886?
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
The Uses of MK-886
MK-886 is a potent and selective inhibitor of FLAP and Cox-1.
The Uses of MK-886
Binds to 5-lipoxygenase-activating protein with high affinity and prevents the activation of 5-lipoxygenase, thus inhibiting the biosynthesis of leukotrienes.
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
Properties of MK-886
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. |
Safety information for MK-886
Computed Descriptors for MK-886
New Products
Tubulysin H Tubulysin F Tubulysin G 2,2-diethoxyethanethioamide 4,4-DIFLUOROPIPERIDINE 2,2-Difluoropropylamine hydrochloride Methyl (R)-1-Boc-4,4-difluoropyrrolidine-2-carboxylate CYCLOBUTYLAMINE HYDROCHLORIDE 2,2-Difluoropropanol 2-(azetidin-3-ylidene)acetonitrile (hydrochloride) Calcium Sodium Phosphosilicate IH (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine Fuel shell 2-(1-(Mercaptomethyl) cyclopropyl) acetonitrile 2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol Imeglimin Hydrochloride IH Magnesium Trisilicate Latanoprostene Bunod Lubiprostone Flame Retardant Zinc Borate (R)-(3-(3-fluoro-4- thiomorpholinophenyl)-2- oxooxazolidin-4-yl) methyl methanesulfonate methyl 3-fluoro-4- thiomorpholino phenylcarbamate 1H-Imidazole-4-carbonitrile 7-Methoxyquinoline-4-carboxylic acidRelated products of tetrahydrofuran
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