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MK 886

Cat. No. M3728
MK 886 Structure
Synonym:

L-663536

Size Price Availability Quantity
5mg USD 80 In stock
10mg USD 135 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

MK 886 inhibits leukotriene biosynthesis (IC50 = 2.5 nM) in vitro and tumor activity in vivo. Displays PPARα antagonist activity. Orally active in vivo. MK-886, has been described that blocks the synthesis of leukotrienes in intact activated leukocytes, but has little or no effect on enzymes involved in leukotriene synthesis, including 5-lipoxygenase, in cell-free systems. MK 886 is a potent inhibitor of leukotriene biosynthesis both in vitro and in vivo indicating that the compound is suitable for studying the role of leukotrienes in a variety of pathological situations. MK 886 inhibited A23187-induced LTB4 formation by rat peripheral blood and elicited PMN.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 472.08
Formula C27H34ClNO2S
CAS Number 118414-82-7
Purity >99%
Solubility DMSO 100 mg/mL
Ethanol 5 mg/mL
Storage at -20°C
References

Inhibition of peroxisome-proliferator-activated receptor (PPAR)alpha by MK886.
Kehrer JP, et al. Biochem J. 2001 Jun 15;356(Pt 3):899-906. PMID: 11389700.

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.
Gillard J, et al. Can J Physiol Pharmacol. 1989 May;67(5):456-64. PMID: 2548691.

Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis.
Dixon RA, et al. Nature. 1990 Jan 18;343(6255):282-4. PMID: 2300173.

5-Lipoxygenase-activating protein is the target of a novel hybrid of two classes of leukotriene biosynthesis inhibitors.
Mancini JA, et al. Mol Pharmacol. 1992 Feb;41(2):267-72. PMID: 1538707.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MK 886, L-663536 supplier, Lipoxygenase, inhibitors

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