[CAS NO. 936350-00-4] Fiboflapon

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PRODUCTS SPECIFICATIONS [936350-00-4]

Catalog

HY-15874

Brand

MCE

CAS

936350-00-4

DESCRIPTION [936350-00-4]

Overview

MDL	-
Molecular Weight	637.83
Molecular Formula	C38H43N3O4S
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

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

Summary

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 IC ₅₀ of 76 nM for inhibition of LTB4 in human blood ^[1] .

IC50 & Target

LTB ₄

76 nM (IC ₅₀ )

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 EC ₅₀ 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 ED ₅₀ s 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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01318980	GlaxoSmithKline	Asthma	September 30, 2010	Phase 1
NCT00955383	GlaxoSmithKline	Asthma	August 14, 2009	Phase 1
NCT01471665	GlaxoSmithKline	Asthma	June 2011	Phase 2
NCT00812773	GlaxoSmithKline	Asthma	December 2008	Phase 2
NCT01156792	GlaxoSmithKline	Asthma	September 2010	Phase 2
NCT01286844	GlaxoSmithKline	Asthma	November 2010	Phase 2
NCT02224521	GlaxoSmithKline	Asthma	April 20, 2009	Phase 1
NCT01147744	GlaxoSmithKline	Asthma	June 28, 2010	Phase 2
NCT01248975	GlaxoSmithKline	Asthma	December 2010	Phase 2
NCT01721135	GlaxoSmithKline	Asthma	September 2010	Phase 1
NCT01411111	GlaxoSmithKline	Asthma	January 6, 2011	Phase 1
NCT00812929	GlaxoSmithKline	Asthma	December 1, 2008	Phase 2
NCT00748306	GlaxoSmithKline	Asthma	December 2008	Phase 2

Appearance

Solid

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)

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 available by MCE.