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Tocris/MK 886/1311/10/10 mg

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货号: 1311

品牌: Tocris

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Description: Inhibitor of 5-lipoxygenase-activating protein (FLAP)

Alternative Names: L-663,536

Chemical Name: 1-[(4-Chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-α,α-dimethyl-5-(1-methylethyl)-1H-Indole-2-propanoic acid

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

An inhibitor of leukotriene biosynthesis (IC₅₀ = 3 nM in human polymorphonuclear leukocytes). Acts by inhibiting 5-lipoxygenase-activating protein (FLAP) (IC₅₀ = 30 nM for inhibition of [¹²⁵I]-L-691,678 photoaffinity labelling). Also moderately potent PPARα antagonist (IC₅₀ = 0.5-1 μM). Orally active in vivo.

Technical Data

M. Wt	472.08
Formula	C₂₇H₃₄ClNO₂S
Storage	Store at RT
Purity	≥98% (HPLC)
CAS Number	118414-82-7
PubChem ID	3651377
InChI Key	QAOAOVKBIIKRNL-UHFFFAOYSA-N
Smiles	ClC(C=C3)=CC=C3CN(C(CC(C)(C(O)=O)C)=C2SC(C)(C)C)C1=C2C=C(C(C)C)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	47.21	100
	ethanol	2.36	5

Preparing Stock Solutions

The following data is based on the product molecular weight 472.08. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.12 mL	10.59 mL	21.18 mL
5 mM	0.42 mL	2.12 mL	4.24 mL
10 mM	0.21 mL	1.06 mL	2.12 mL
50 mM	0.04 mL	0.21 mL	0.42 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Dixon et al (1990) Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis. Nature 343 282 PMID: 2300173

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 PMID: 2548691

Kehrer et al (2001) Inhibition of peroxisome-proliferator-activated receptor (PPAR)α by MK886. Biochem.J. 356 899 PMID: 11389700

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

Keywords: MK 886, supplier, Inhibitor, 5-lipoxygenase-activating, protein, FLAP, PPARα, PPARalpha, antagonists, inhibitors, inhibits, Oxygenases, Oxidases, leukotrienes, eicosanoids, biosynthesis, Peroxisome, Proliferator-activated, PPARs, MK886, L663536, 5-LOX, L-663,536, Lipoxygenase, Tocris Bioscience

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