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

Fiboflapon (Synonyms: GSK2190915; AM-803)

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

Fiboflapon (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 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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200 mg   Get quote  

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Description

Fiboflapon (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 (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 803FLAPLeukotriene Receptor5-lipoxygenase-activating protein5-LO activating proteinInhibitorinhibitorinhibit

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Product name:
Fiboflapon
Cat. No.:
HY-15874
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