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
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
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..…
N-Bromosuccinimide Price
- Product number
- 28600
- Product name
- GSK2190915
- Packaging
- 1mg
- Price
- $110
- Updated
- 2024/03/01
- Product number
- CS-3604
- Product name
- Fiboflapon
- Purity
- 98.18%
- Packaging
- 5mg
- Price
- $151
- Updated
- 2021/12/16
- Product number
- 8831BB
- Product name
- Fiboflapon
- Packaging
- 1mg
- Price
- $220
- Updated
- 2021/12/16
- Product number
- CS-3604
- Product name
- Fiboflapon
- Purity
- 98.18%
- Packaging
- 10mg
- Price
- $252
- Updated
- 2021/12/16
- Product number
- INB0001116
- Product name
- AM-803
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $504.75
- Updated
- 2021/12/16
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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