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AM103

Catalog No. T10314   CAS 1147872-22-7
Synonyms: AM 103

AM103 is an effective and selective inhibitor of FLAP (IC50 = 4.2 nM).

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AM103 Chemical Structure
AM103, CAS 1147872-22-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 183.00
2 mg In stock $ 273.00
5 mg In stock $ 463.00
10 mg In stock $ 683.00
25 mg In stock $ 1,070.00
50 mg In stock $ 1,450.00
100 mg In stock $ 1,950.00
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Purity: 99.21%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description AM103 is an effective and selective inhibitor of FLAP (IC50 = 4.2 nM).
Targets&IC50 FLAP:4.2 nM
In vitro AM103 is against the 5 most common CYP isoforms with IC50s >30 μM for CYP2D6 and >50 μM for CYP3A4, CYP2C9, CYP2C19, and CYP1A2[1]. AM103 shows IC50s of 350, 113, and 117 nM against human, rat, and mouse whole-blood ionophore-stimulated LTB4 production, respectively[2].
In vivo AM103 has high bioavailability of 64%, low clearance of 2.9 mL/min/kg, low volume of distribution of 0.41 L/kg, and a long i.v. half-life of 5.2 h in dogs. AM103 (10 mg/kg) inhibits the increase in CysLTs and EPO by approximately 60% and reduces the level of IL-5[1]. In a model of chronic lung inflammation using ovalbumin-primed and challenged BALB/c mice, AM103 reduces eosinophil peroxidase, CysLTs, and IL-5 in the bronchoalveolar lavage fluid. AM103 increases survival time in mice exposed to a lethal intravenous injection of platelet-activating factor. In the rat lung challenged in vivo with calcium ionophore, AM103 inhibits LTB4 and cysteinyl leukotriene production with ED50 values of 0.8 and 1 mg/kg, respectively[2].
Synonyms AM 103
Molecular Weight 631.76
Formula C36H38N3NaO4S
CAS No. 1147872-22-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 180 mg/mL (284 mM), sonification is recommended.

TargetMolReferences and Literature

1. Hutchinson JH, et al. 5-lipoxygenase-activating protein inhibitors: development of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103). J Med Chem. 2009 Oct 8;52(19):5803-15. 2. Lorrain DS, et al. Pharmacological characterization of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103), a novel selective 5-lipoxygenase-activating protein inhibitor that reduces acute and chronic inflammation. J Pharmacol Exp Ther. 2009 Dec;331(3):1042-50.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library

Related Products

Related compounds with same targets
Quiflapon sodium Quiflapon sEH/FLAP-IN-1 Atuliflapon LTB4-IN-2 Diflapolin FEN1-IN-7 FEN1-IN-6

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Keywords

AM103 1147872-22-7 Immunology/Inflammation FLAP AM-103 AM 103 inhibitor inhibit

 

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