MK-0591 (Synonyms: L-686,708, Quiflapon) |
| Catalog No.GC11457 |
An inhibitor of FLAP
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 136668-42-3
Sample solution is provided at 25 µL, 10mM.
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MK-0591, an analog of MK-886 is a potent and orally active leukotriene biosynthesis inhibitor with an IC50 value of 600 ng/ml.
MK-0591(250 mg) nearly completely inhibited systemic leukotriene synthesis (>90%) in whole blood or in patients with active disease, and induced LTB4 synthesis in the target tissue of inflammation. [1]
MK-0591 plays as a potential agent for the treatment of asthma and inflammatory bowel disease. MK-0591 specific interacted with 5-lipoxygenase, a membrane protein activating protein FLAP, which is essential for LT synthesis in inflammatory cells. [3]
MK-0591 inhibited 96% production of LTB4 in whole blood and 91% that from BAL cells. By contrast, MK-0591 had no effect on airway hyper-responsiveness, ozone-induced bronchoconstriction, or influx of neutrophils into BAL. [4]
References:
1.Hillingsø J, Kjeldsen J, Laursen LS et al. Blockade of leukotriene production by a single oral dose of MK-0591 in active ulcerative colitis. Clin Pharmacol Ther. 1995 Mar;57(3):335-41.
2.Prasit P, Belley M, Blouin M et al. A new class of leukotriene biosynthesis inhibitor: the development of MK-0591. J Lipid Mediat. 1993 Mar-Apr;6(1-3):239-44.
3.Stevens WH, Lane CG, Woolley MJ et al. Effect of FLAP antagonist MK-0591 on leukotriene production and ozone-induced airway responses in dogs. J Appl Physiol (1985). 1994 Apr;76(4):1583-8.
| Cas No. | 136668-42-3 | SDF | |
| Sinónimos | L-686,708, Quiflapon | ||
| Chemical Name | 3-[3-tert-butylsulfanyl-1-[(4-chlorophenyl)methyl]-5-(quinolin-2-ylmethoxy)indol-2-yl]-2,2-dimethylpropanoic acid | ||
| Canonical SMILES | CC(C)(C)SC1=C(N(C2=C1C=C(C=C2)OCC3=NC4=CC=CC=C4C=C3)CC5=CC=C(C=C5)Cl)CC(C)(C)C(=O)O | ||
| Formula | C34H35ClN2O3S | M.Wt | 587.17 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7031 mL | 8.5154 mL | 17.0308 mL |
| 5 mM | 0.3406 mL | 1.7031 mL | 3.4062 mL |
| 10 mM | 0.1703 mL | 0.8515 mL | 1.7031 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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