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MedKoo Cat#: 319748 | Name: Fiboflapon
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Fiboflapon, also known as AM-803 and GSK2190915, is a potent, oral, once daily FLAP inhibitor (5-lipoxygenase-activating protein inhibitor). GSK2190915 attenuated the early (0-2 h) and late (4-10 h) asthmatic responses to inhaled allergen compared with placebo. GSK2190915 shows potential as a treatment for patients with asthma. Efficacy was demonstrated for GSK2190915 30 mg compared with placebo in day-time symptom scores and day-time SABA use.

Chemical Structure

Fiboflapon
Fiboflapon
CAS#936350-00-4 (free acid)

Theoretical Analysis

MedKoo Cat#: 319748

Name: Fiboflapon

CAS#: 936350-00-4 (free acid)

Chemical Formula: C38H43N3O4S

Exact Mass: 637.2974

Molecular Weight: 637.84

Elemental Analysis: C, 71.56; H, 6.80; N, 6.59; O, 10.03; S, 5.03

Price and Availability

Size Price Availability Quantity
5mg USD 350.00 2 Weeks
10mg USD 650.00 2 Weeks
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Related CAS #
1196070-26-4 (sodium) 936350-00-4 (free acid)
Synonym
AM-803; AM 803; AM803; GSK2190915; GSK-2190915; GSK 2190915; Fiboflapon; fiboflaponum
IUPAC/Chemical Name
3-(3-(tert-butylthio)-1-(4-(6-ethoxypyridin-3-yl)benzyl)-5-((5-methylpyridin-2-yl)methoxy)-1H-indol-2-yl)-2,2-dimethylpropanoic acid
InChi Key
DFQGDHBGRSTTHX-UHFFFAOYSA-N
InChi Code
InChI=1S/C38H43N3O4S/c1-8-44-34-18-14-28(22-40-34)27-12-10-26(11-13-27)23-41-32-17-16-30(45-24-29-15-9-25(2)21-39-29)19-31(32)35(46-37(3,4)5)33(41)20-38(6,7)36(42)43/h9-19,21-22H,8,20,23-24H2,1-7H3,(H,42,43)
SMILES Code
O=C(O)C(C)(C)CC(N1CC2=CC=C(C3=CC=C(OCC)N=C3)C=C2)=C(SC(C)(C)C)C4=C1C=CC(OCC5=NC=C(C)C=C5)=C4
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 637.84 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Chaudhuri R, Norris V, Kelly K, Zhu CQ, Ambery C, Lafferty J, Cameron E, Thomson NC. Effects of a FLAP inhibitor, GSK2190915, in asthmatics with high sputum neutrophils. Pulm Pharmacol Ther. 2014 Feb;27(1):62-9. doi: 10.1016/j.pupt.2013.11.007. Epub 2013 Dec 10. PMID: 24333186. 2: Kent SE, Bentley JH, Miller D, Sterling R, Menendez R, Tarpay M, Pearlman DS, Norris V. The effect of GSK2190915, a 5-lipoxygenase-activating protein inhibitor, on exercise-induced bronchoconstriction. Allergy Asthma Proc. 2014 Mar-Apr;35(2):126-33. doi: 10.2500/aap.2014.35.3723. PMID: 24717789. 3: Bain G, King CD, Schaab K, Rewolinski M, Norris V, Ambery C, Bentley J, Yamada M, Santini AM, van de Wetering de Rooij J, Stock N, Zunic J, Hutchinson JH, Evans JF. Pharmacodynamics, pharmacokinetics and safety of GSK2190915, a novel oral anti-inflammatory 5-lipoxygenase-activating protein inhibitor. Br J Clin Pharmacol. 2013 Mar;75(3):779-90. doi: 10.1111/j.1365-2125.2012.04386.x. PMID: 22803688; PMCID: PMC3575944. 4: Kent SE, Boyce M, Diamant Z, Singh D, O'Connor BJ, Saggu PS, Norris V. The 5-lipoxygenase-activating protein inhibitor, GSK2190915, attenuates the early and late responses to inhaled allergen in mild asthma. Clin Exp Allergy. 2013 Feb;43(2):177-86. doi: 10.1111/cea.12002. PMID: 23331559. 5: Follows RM, Snowise NG, Ho SY, Ambery CL, Smart K, McQuade BA. Efficacy, safety and tolerability of GSK2190915, a 5-lipoxygenase activating protein inhibitor, in adults and adolescents with persistent asthma: a randomised dose- ranging study. Respir Res. 2013 May 17;14(1):54. doi: 10.1186/1465-9921-14-54. PMID: 23682661; PMCID: PMC3732081. 6: Mosteller M, Condreay LD, Harris EC, Ambery C, Beerahee M, Ghosh S. Exploring the roles of UGT1A1 and UGT1A3 in oral clearance of GSK2190915, a 5-lipoxygenase-activating protein inhibitor. Pharmacogenet Genomics. 2014 Dec;24(12):618-21. doi: 10.1097/FPC.0000000000000090. PMID: 25192553. 7: Singh D, Boyce M, Norris V, Kent SE, Bentley JH. Inhibition of the early asthmatic response to inhaled allergen by the 5-lipoxygenase activating protein inhibitor GSK2190915: a dose-response study. Int J Gen Med. 2013 Dec 9;6:897-903. doi: 10.2147/IJGM.S51364. PMID: 24357936; PMCID: PMC3862733. 8: Snowise NG, Clements D, Ho SY, Follows RM. Addition of a 5-lipoxygenase- activating protein inhibitor to an inhaled corticosteroid (ICS) or an ICS/long- acting beta-2-agonist combination in subjects with asthma. Curr Med Res Opin. 2013 Dec;29(12):1663-74. doi: 10.1185/03007995.2013.842163. Epub 2013 Sep 19. PMID: 24010736. 9: Xia C, Sadeghi L, Strååt K, Merrien M, Wright AP, Sander B, Xu D, Österborg A, Björkholm M, Claesson HE. Intrinsic 5-lipoxygenase activity regulates migration and adherence of mantle cell lymphoma cells. Prostaglandins Other Lipid Mediat. 2021 Oct;156:106575. doi: 10.1016/j.prostaglandins.2021.106575. Epub 2021 Jun 8. PMID: 34116165. 10: Mashima R, Okuyama T. The role of lipoxygenases in pathophysiology; new insights and future perspectives. Redox Biol. 2015 Dec;6:297-310. doi: 10.1016/j.redox.2015.08.006. Epub 2015 Aug 7. PMID: 26298204; PMCID: PMC4556770. 11: Sampson AP. FLAP inhibitors for the treatment of inflammatory diseases. Curr Opin Investig Drugs. 2009 Nov;10(11):1163-72. PMID: 19876784. 12: Stock NS, Bain G, Zunic J, Li Y, Ziff J, Roppe J, Santini A, Darlington J, Prodanovich P, King CD, Baccei C, Lee C, Rong H, Chapman C, Broadhead A, Lorrain D, Correa L, Hutchinson JH, Evans JF, Prasit P. 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 daily FLAP inhibitor. J Med Chem. 2011 Dec 8;54(23):8013-29. doi: 10.1021/jm2008369. Epub 2011 Nov 7. PMID: 22059882. 13: Lorrain DS, Bain G, Correa LD, Chapman C, Broadhead AR, Santini AM, Prodanovich PP, Darlington JV, Stock NS, Zunic J, King CD, Lee C, Baccei CS, Stearns B, Roppe J, Hutchinson JH, Prasit P, Evans JF. 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. doi: 10.1016/j.ejphar.2010.05.003. Epub 2010 May 21. PMID: 20519143.

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