MK-886 sodium salt CAS: 118427-55-7
MF: C27H33ClNO2S•Na
MW: 494.06
A potent and selective inhibitor of FLAP and Cox-1.

MK-886 sodium salt (CAS 118427-55-7)

MK-886 sodium salt | CAS 118427-55-7 is rated 5.0 out of 5 by 1.
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Synonym: 3-[1-(p-Chlorobenzyl)-5-(isopropyl)-3-t-butylthioindol-2-yl]-2,2-dimethylpropanoic acid . Na
Application: A potent and selective inhibitor of FLAP and Cox-1
CAS Number: 118427-55-7
Purity: ≥98%
Molecular Weight: 494.06
Molecular Formula: C27H33ClNO2S•Na
* Refer to Certificate of Analysis for lot specific data (including water content).
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MK-886 sodium salt, also designated L-663,536, is a potent and selective inhibitor of 5-lipoxygenase-activating protein (FLAP). FLAP is an arachidonic acid binding protein that is critical in the biosynthesis of leukotrienes. Inhibitors of FLAP prevent translocation of 5-lipoxygenase from the cytosol to the membrane and inhibit 5-lipoxygenase (5-LO) activation. MK-886 binds to FLAP with high affinity and prevents the activation of 5-LO, thus inhibiting leukotriene biosynthesis: 2.5 nM in intact leukocytes; 1.1 µM in whole blood. MK-886 sodium salt is an inhibitor of Cox-1, PGE Synthase and PPARα.


References

1. Gillard, J., et al. 1989. Can. J. Physiol. Pharmacol. 67: 456-464. PMID: 2548691
2. Dixon, R.A., et al. 1990. Nature. 343: 282-284. PMID: 2300173
3. Ford-Hutchinson, A.W., 1991. Trends Pharmacol. Sci. 12: 68-70. PMID: 2024291

Physical State :
Solid
Solubility :
Soluble in 100%ethanol (25 mg/ml), DMSO (25 mg/ml), a 1:4 solution of DMF:PBS(pH7.2) (~0.2 mg/ml), DMF (~20 mg/ml), and water (0.2 mg/ml) at 25° C.
Storage :
Store at room temperature
IC50 :
leukotriene: IC50 = 2.5 nM (leukocytes); leukotriene: IC50 = 1.1 µM ( human whole blood)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
4519262
MDL Number :
MFCD11045945
SMILES :
CC(C)C1=CC2=C(C=C1)N(C(=C2SC(C)(C)C)CC(C)(C)C(=O)[O-])CC3=CC=C(C=C3)Cl.[Na+]

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Certificate of Analysis

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MK-886 sodium salt  Product Citations

See how others have used MK-886 sodium salt. Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

PMID: # 25362851  Xu, Y. et al. 2015. Oncogene. 34: 4229-37.

PMID: # 24167735  Al-Amran, FG. et al. 2013. ISRN Pharmacol. 2013: 303717.

PMID: # 23535410  Takeda, S. et al. 2013. J Toxicol Sci. 38: 305-8.

Citations 1 to 3 of 3 total
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Rated 5 out of 5 by from Hawkes Hawkes, CA. et al. (PubMed 24021653) reported that MK-886, an inhibitor of FLAP and Cox-1, reduces cerebral amyloid angiopathy severity in TgCRND8 mice. -SCBT Publication Review
Date published: 2015-02-11
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