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AM103 is an effective and selective inhibitor of FLAP (IC50 = 4.2 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 138 € | In Stock | |
5 mg | 344 € | In Stock | |
10 mg | 518 € | In Stock | |
25 mg | 933 € | In Stock | |
50 mg | 1.301 € | In Stock | |
100 mg | 1.786 € | In Stock |
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]. |
Alias | AM 103 |
Molecular Weight | 631.76 |
Formula | C36H38N3NaO4S |
Cas No. | 1147872-22-7 |
Smiles | [Na+].COc1ccc(cn1)-c1ccc(Cn2c(CC(C)(C)C([O-])=O)c(SC(C)(C)C)c3cc(OCc4ccccn4)ccc23)cc1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 180 mg/mL (284 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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