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[CAS NO. 936350-00-4] Fiboflapon
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15874 |
| Brand: | MCE |
| CAS: | 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 |
Summary
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
DMSO : 50 mg/mL ( 78.39 mM ; Need ultrasonic)
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 |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (3.92 mM); Clear solution
References
- [1] Stock NS, et al. 5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once
- [2] Lorrain DS, et al. Pharmacology of AM803, a novel selective five-lipoxygenase-activating protein (FLAP) inhibitor in rodent models of acute inflammation. Eur J Pharmacol. 2010 Aug 25;640(1-3):211-8.
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