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GSK2190915

Chemical Structure : GSK2190915

CAS No.: 936350-00-4

GSK2190915 (AM-803;Fiboflapon;GSK-2190915)

Catalog No.: PC-44768Not For Human Use, Lab Use Only.

Fiboflapon (AM-803, GSK 2190915) is a potent, selective 5-lipoxygenase-activating protein (FLAP) inhibitor with binding IC50 of 2.6 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Fiboflapon (AM-803, GSK 2190915) is a potent, selective 5-lipoxygenase-activating protein (FLAP) inhibitor with binding IC50 of 2.6 nM.
Fiboflapon (AM-803, GSK 2190915) inhibits LTB4 synthesis following ionophore challenge in human whole blood with IC50 of 76 nM (5 h incubation).
Fiboflapon (AM-803, GSK 2190915) shows good selectivity over CYP3A4, 2C9, and 2D6.
Fiboflapon (AM-803, GSK 2190915) exhibits excellent preclinical toxicology, pharmacokinetics and oral bioactivity.

Physicochemical Properties

M.Wt 637.8307
Formula C38H43N3O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1H-Indole-2-propanoic acid, 3-[(1,1-dimethylethyl)thio]-1-[[4-(6-ethoxy-3-pyridinyl)phenyl]methyl]-α,α-dimethyl-5-[(5-methyl-2-pyridinyl)methoxy]-

References

1. Stock NS, et al. J Med Chem. 2011 Dec 8;54(23):8013-29.

2. Lorrain DS, et al. Eur J Pharmacol. 2010 Aug 25;640(1-3):211-8.

3. Kent SE, et al. Clin Exp Allergy. 2013 Feb;43(2):177-86.

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