GSK2190915

Product Name: GSK2190915
CAS No.: 936350-00-4
Chemical Name: GSK2190915
Synonyms: AM 803;GSK2190915;fiboflapon;GSK2190915 (AM803);Fiboflapon (GSK2190915);Fiboflapon, 10 mM in DMSO;AM-803;FIBOFLAPON;GSK-2190915;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;1H-Indole-2-propanoic acid, 3-[(1,1-dimethylethyl)thio]-1-[[4-(6-ethoxy-3-pyridinyl)phenyl]methyl]-α,α-dimethyl-5-[(5-methyl-2-pyridinyl)methoxy]-;3-[(1,1-Dimethylethyl)thio]-1-[[4-(6-ethoxy-3-pyridinyl)phenyl]methyl]-alpha,alpha-dimethyl-5-[(5-methyl-2-pyridinyl)methoxy]-1H-indole-2-propanoic acid
CBNumber: CB02735522
Molecular Formula: C38H43N3O4S
Formula Weight: 637.83
MOL File: 936350-00-4.mol

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GSK2190915 Property

Boiling point:: 796.3±60.0 °C(Predicted)
Density: 1.16±0.1 g/cm3(Predicted)
solubility: DMSO: soluble; Methanol: soluble
form: A crystalline solid
pka: 4.70±0.10(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H361Suspected of damaging fertility or the unborn child

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P281Use personal protective equipment as required.

P308+P313IF exposed or concerned: Get medical advice/attention.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 28600
Product name: GSK2190915
Packaging: 1mg
Price: $110
Updated: 2024/03/01

ChemScene

Product number: CS-3604
Product name: Fiboflapon
Purity: 98.18%
Packaging: 5mg
Price: $151
Updated: 2021/12/16

AK Scientific

Product number: 8831BB
Product name: Fiboflapon
Packaging: 1mg
Price: $220
Updated: 2021/12/16

ChemScene

Product number: CS-3604
Product name: Fiboflapon
Purity: 98.18%
Packaging: 10mg
Price: $252
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: INB0001116
Product name: AM-803
Purity: 95.00%
Packaging: 5MG
Price: $504.75
Updated: 2021/12/16

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GSK2190915 Chemical Properties,Usage,Production

Uses

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].

Definition

ChEBI: Fiboflapon is a phenylpyridine.

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].

IC 50

LTB₄: 76 nM (IC₅₀)

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 DOI:10.1021/jm2008369
[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. DOI:10.1016/j.ejphar.2010.05.003

GSK2190915 Preparation Products And Raw materials

Raw materials

Preparation Products

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GSK2190915 Suppliers

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936350-00-4, GSK2190915Related Search:

GSK2190915

GSK2190915 (AM803)

fiboflapon

AM 803

3-[(1,1-Dimethylethyl)thio]-1-[[4-(6-ethoxy-3-pyridinyl)phenyl]methyl]-alpha,alpha-dimethyl-5-[(5-methyl-2-pyridinyl)methoxy]-1H-indole-2-propanoic acid

AM-803;FIBOFLAPON;GSK-2190915

1H-Indole-2-propanoic acid, 3-[(1,1-dimethylethyl)thio]-1-[[4-(6-ethoxy-3-pyridinyl)phenyl]methyl]-α,α-dimethyl-5-[(5-methyl-2-pyridinyl)methoxy]-

Fiboflapon, 10 mM in DMSO

Fiboflapon (GSK2190915)

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

936350-00-4

C38H43N3O4S