1. Immunology/Inflammation
    GPCR/G Protein
  2. FLAP
    Leukotriene Receptor
  3. Fiboflapon sodium

Fiboflapon sodium (Synonyms: GSK2190915 sodium salt; AM-803 sodium)

Cat. No.: HY-15874A Purity: 99.08%
Handling Instructions

Fiboflapon sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.

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

Fiboflapon sodium Chemical Structure

Fiboflapon sodium Chemical Structure

CAS No. : 1196070-26-4

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10 mM * 1 mL in DMSO USD 219 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 sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood[1].

IC50 & Target[1]

LTB4

76 nM (IC50)

In Vitro

Fiboflapon (AM803) exhibits excellent preclinical toxicology and pharmacokinetics in rat and dog. Fiboflapon (AM803) also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model[1]. Oral administration of Fiboflapon (AM803) (1 mg/kg) resulted 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 were challenged in vivo with calcium-ionophore, Fiboflapon (AM803) inhibited 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 (AM803) dose-dependently reduced LTB4, CysLTs, plasma protein extravasation and neutrophil influx induced by peritoneal zymosan injection. Finally, AM803 increased survival time in mice exposed to a lethal intravenous injection of platelet activating factor (PAF)[2].

Clinical Trial
Molecular Weight

659.81

Formula

C₃₈H₄₂N₃NaO₄S

CAS No.

1196070-26-4

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.[Na+]

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 : ≥ 32 mg/mL (48.50 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5156 mL 7.5779 mL 15.1559 mL
5 mM 0.3031 mL 1.5156 mL 3.0312 mL
10 mM 0.1516 mL 0.7578 mL 1.5156 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

FiboflaponGSK2190915AM-803GSK 2190915GSK-2190915AM803AM 803FLAPLeukotriene Receptor5-lipoxygenase-activating protein5-LO activating proteinInhibitorinhibitorinhibit

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Fiboflapon sodium
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HY-15874A
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