3-[1-(4-Chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
MK-886
CAS: 118414-82-7
Molecular Formula: C27H34ClNO2S
3-[1-(4-Chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid - Names and Identifiers
3-[1-(4-Chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid - Physico-chemical Properties
| Molecular Formula | C27H34ClNO2S |
| Molar Mass | 472.08 |
| Melting Point | 295-297°C |
| Solubility | DMSO: 47.2 mg/mL (100 mM)Ethanol: 2.4 mg/mL (5 mM)( < 1 mg/ml refers to the product slightly soluble or insoluble) |
| Appearance | White solid. |
| Color | white |
| Storage Condition | Sealed in dry,2-8°C |
| Stability | Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months. |
| Use | MK-886 (L 663536) is an effective, cell-permeable and orally active inhibitor of FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50 of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively). MK-886 is also a non-competitive PPARα antagonist, which can induce apoptosis. |
| Target | COX-1; COX-2 |
| In vitro study | MK-886, lipoxygenase activating protein (FLAP) inhibitors, in intact cells can effectively inhibit leukotriene biosynthesis. MK-886 are frequently used to identify the role of the 5-lipoxygenase pathway in cellular and animal models of inflammation, allergy, cancer, and cardiovascular disease. MK-886 inhibition of COX-1(IC50 = 8 μm) and, the formation of the COX-1 derivatives 12-HHT and thromboxane B2 was prevented (IC50=13-15 μm), while the effect on COX-2 was relatively small (IC50=58 μm). In A549 cells, MK-886(33 μm) did not inhibit COX2-dependent formation of 6-ketoprostaglandin (PG)F1α. MK-886(10 μm) inhibited COX-1 mediated platelet aggregation after collagen and arachidonic acid induction, but did not affect thrombin, U-46619 induced aggregation. |
| In vivo study | After repeated daily injections of MK-886 into the peritoneal cavity of the mice, GluR1 phosphorylation was elevated in the brain tissue of the prefrontal cortex. In contrast, a single injection of MK-886 did not affect cortical GluR1 phosphorylation. |
3-[1-(4-Chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid - Risk and Safety
| WGK Germany | 3 |
3-[1-(4-Chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.024 ml | 10.12 ml | 20.24 ml |
| 5 mM | 0.405 ml | 2.024 ml | 4.048 ml |
| 10 mM | 0.202 ml | 1.012 ml | 2.024 ml |
| 5 mM | 0.04 ml | 0.202 ml | 0.405 ml |
Last Update：2024-01-02 23:10:35
3-[1-(4-Chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid - Cell Experiment
IL-1β-stimulated A549 cells (5×106/ml) are pre-incubated with MK-886 (MK, 33 μM), indomethacin (Indo, 10 μM), celecoxib (Cele, 5 μM) or vehicle (DMSO) for 15 min prior to the addition of 30 μM arachidonic acid. After 15 min at 37°C the amount of released 6-keto PGF1α was assessed by ELISA as determined in the Materials and methods section. (Only for Reference) cell line: A549 cells
Last Update：2023-08-16 21:32:38
3-[1-(4-Chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid - Animal Experiment
Animal model: C57BL/6J mice
Last Update：2023-08-16 21:32:38
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Spot supply
Product Name: MK-886 Visit Supplier Webpage Request for quotationCAS: 118414-82-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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