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GSK2190915

Cat. No. M2733
GSK2190915 Structure
Synonym:

AM-803, Fiboflapon

Size Price Availability
5mg USD 150  USD150 Out of stock
10mg USD 250  USD250 Out of stock
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Quality Control & Documentation
Biological Activity

GSK2190915 (AM803), a potent FLAP inhibitor, prevents the synthesis of leukotrienes and 5-oxo-ETE, with IC50 of 76 nM for inhibition of LTB4 in human blood, provides treatment for asthma.

Chemical Information
Molecular Weight 637.83
Formula C38H43N3O4S
CAS Number 936350-00-4
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Sandra E Kent, et al. The effect of GSK2190915, a 5-lipoxygenase-activating protein inhibitor, on exercise-induced bronchoconstriction

[2] R Chaudhuri, et al. Effects of a FLAP inhibitor, GSK2190915, in asthmatics with high sputum neutrophils

[3] Richard M A Follows, et al. Efficacy, safety and tolerability of GSK2190915, a 5-lipoxygenase activating protein inhibitor, in adults and adolescents with persistent asthma: a randomised dose-ranging study

[4] S E Kent, et al. The 5-lipoxygenase-activating protein inhibitor, GSK2190915, attenuates the early and late responses to inhaled allergen in mild asthma

[5] Gretchen Bain, et al. Pharmacodynamics, pharmacokinetics and safety of GSK2190915, a novel oral anti-inflammatory 5-lipoxygenase-activating protein inhibitor

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Keywords: GSK2190915, AM-803, Fiboflapon supplier, Lipoxygenase, inhibitors, activators


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