1. Immunology/Inflammation
  2. FLAP
  3. Fiboflapon

Fiboflapon (Synonyms: GSK2190915; AM-803)

Cat. No.: HY-15874 Purity: 98.18%
Handling Instructions

Fiboflapon (GSK2190915) is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor with binding IC50 of 2.9 nM.

For research use only. We do not sell to patients.

Fiboflapon Chemical Structure

Fiboflapon Chemical Structure

CAS No. : 936350-00-4

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 212 In-stock
Estimated Time of Arrival: December 31
5 mg USD 151 In-stock
Estimated Time of Arrival: December 31
10 mg USD 252 In-stock
Estimated Time of Arrival: December 31
50 mg USD 994 In-stock
Estimated Time of Arrival: December 31
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Description

Fiboflapon (GSK2190915) is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor with binding IC50 of 2.9 nM.

IC50 & Target

IC50: 76 nM (inhibition of LTB4 in human blood 5 h incubation)[1].

In Vitro

Fiboflapon (AM-803) exhibits excellent preclinical toxicology and pharmacokinetics in rat and dog. Fiboflapon (AM-803) also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model [1].

In Vivo

Oral administration of Fiboflapon (AM-803: 1 mg/kg) results in sustained inhibition of ex vivo ionophore-challenged whole blood LTB4 biosynthesis with >90% inhibition for up to 12 h and an EC50 of approximately 7 nM. When rat lungs are challenged in vivo with calcium-ionophore, Fiboflapon (AM-803) inhibits LTB4 and cysteinyl leukotriene (CysLT) production with ED50s of 0.12 mg/kg and 0.37 mg/kg, respectively. The inhibition measured 16 h following a single oral dose of 3 mg/kg was 86% and 41% for LTB4 and CysLTs, respectively. In an acute inflammation setting, Fiboflapon dose-dependently reduced LTB4, CysLTs, plasma protein extravasation and neutrophil influx induced by peritoneal zymosan injection. Finally, Fiboflapon increases survival time in mice exposed to a lethal intravenous injection of platelet activating factor (PAF)[1].

Clinical Trial
Molecular Weight

637.83

Formula

C₃₈H₄₃N₃O₄S

CAS No.

936350-00-4

SMILES

CC(C(O)=O)(C)CC1=C(SC(C)(C)C)C2=CC(OCC3=CC=C(C)C=N3)=CC=C2N1CC4=CC=C(C5=CN=C(OCC)C=C5)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (78.39 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5678 mL 7.8391 mL 15.6782 mL
5 mM 0.3136 mL 1.5678 mL 3.1356 mL
10 mM 0.1568 mL 0.7839 mL 1.5678 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.92 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

FiboflaponGSK2190915AM-803GSK 2190915GSK-2190915AM803AM 803FLAP5-lipoxygenase-activating protein5-LO activating proteinInhibitorinhibitorinhibit

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Fiboflapon
Cat. No.:
HY-15874
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