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GSK2190915

Cat. No. M2733
GSK2190915 Structure
Synonym:

AM-803, Fiboflapon

Size Price Availability
5mg USD 140  USD140 Out of stock
25mg USD 460  USD460 Out of stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 637.83
Formula C38H43N3O4S
CAS Number 936350-00-4
Purity >98%
Solubility DMSO
Storage at -20°C
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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  Catalog
Abmole Inhibitor Catalog 2017




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

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