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| 5mg |
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| 25mg |
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Purity: ≥98%
MK886 (also known as L663536) is a novel and potent 5-lipoxygenase-activating protein inhibitor and a leukotriene biosynthesis inhibitor (IC50=2.5 nM). MK-886 acts by blocking the 5-lipoxygenase activating protein (FLAP), thus inhibiting 5-lipoxygenase (5-LOX), and may help in treating atherosclerosis. MK-886 inhibits cyclooxygenase-1 activity and suppresses platelet aggregation. MK-886 induces changes in cell cycle and increases apoptosis after photodynamic therapy with hypericin. MK-886 enhances tumour necrosis factor-alpha-induced differentiation and apoptosis.
| ln Vitro |
In primary mouse keratinocyte cultures, MK-886 (0.5-2 μM; 15 hours; primary keratinocytes) treatment decreases keratin-1 expression [1]. 10 μM MK-886 was found to be able to suppress the activation of PPARα by Wy-14643 by around 80% in monkey kidney fibroblast CV-1 cells, mouse keratinocyte 308 cells, and human lung adenocarcinoma A549 cells using a transient transfection technique. In stable transfection systems, MK-886 can also lessen the activation of PPARα by fatty acids [1]. MK-886-induced apoptosis cannot be stopped by PPARα and PPARγ agonists, despite the fact that Jurkat cells express all PPAR isoforms [1].
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| ln Vivo |
Methysergide-pretreated inbred rats' antigen-induced dyspnea is successfully inhibited by MK-886 (L 663536; 5 mg/kg; oral; male Sprague-Dawley rats) treatment [2]. ?In rat pleurisy (ED50, 0.2 mg/kg po), inflammatory paw (ED50, 0.8 mg/kg), and rat biliary leukotriene excretion models, MK-886 (L 663536) reduces leukotriene excretion in vivo. Triene biosynthesis elicitation of antigen [2].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Primary Keratinocytes Tested Concentrations: 0.5 µM, 1 µM or 2 µM Incubation Duration: 15 hrs (hours) Experimental Results: diminished keratin-1 expression. |
| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (300-400 g), antigen-induced dyspnea [1]
Doses: 5 mg/kg Route of Administration: Oral Experimental Results:Inhibition of antigen-induced dyspnea. |
| References |
[1]. Kehrer JP et al. Inhibition of peroxisome-proliferator-activated receptor (PPAR)alpha by MK886. Biochem J. 2001 Jun 15.
[2]. [2] Gillard J et al. 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. 1989 May;67(5):456-64. [3]. Mancini JA, et al. 5-Lipoxygenase-activating protein is the target of a novel hybrid of two classes of leukotriene biosynthesis inhibitors. Mol Pharmacol. 1992 Feb;41(2):267-72. |
| Molecular Formula |
C27H34CLNO2S
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|---|---|
| Molecular Weight |
472.0824
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| CAS # |
118414-82-7
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| Related CAS # |
MK-886 sodium salt;118427-55-7
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| SMILES |
O=C(O)C(C)(C)CC(N1CC2=CC=C(Cl)C=C2)=C(SCCCC)C3=C1C=CC(C(C)C)=C3
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| InChi Key |
VFMGWQLOCZBFCK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H34ClNO2S/c1-6-7-14-32-25-22-15-20(18(2)3)10-13-23(22)29(17-19-8-11-21(28)12-9-19)24(25)16-27(4,5)26(30)31/h8-13,15,18H,6-7,14,16-17H2,1-5H3,(H,30,31)
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| Chemical Name |
3-[3-butylsulfanyl-1-[(4-chlorophenyl)methyl]-5-propan-2-yl-indol-2-yl]-2,2 -dimethyl-propanoic acid
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| Synonyms |
L-663,536; MK 886; L663,536; MK886; L-663536; L 663,536; MK-886; L663536; L 663536.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~75 mg/mL (~158.87 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.30 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (4.41 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10 mg/mL (21.18 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1183 mL | 10.5914 mL | 21.1829 mL | |
| 5 mM | 0.4237 mL | 2.1183 mL | 4.2366 mL | |
| 10 mM | 0.2118 mL | 1.0591 mL | 2.1183 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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