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AM103

CAT: 0013-GTR19216977-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19216977-01Size:200 mg
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Description
AM103 is an effective and selective inhibitor of FLAP (IC50 = 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. AM103 shows IC50s of 350, 113, and 117 nM against human, rat, and mouse whole-blood ionophore-stimulated LTB4 production, respectively. (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. 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.
CAS Number
1147872-22-7
Product Name Alternative
AM 103
Purity
>98% (HPLC)
Solubility
In Vitro: DMSO : 200 mg/mL (316.58 mM)
Smiles
[NaH].COc1ccc (cn1) -c1ccc (Cn2c (CC (C) (C) C (O) =O) c (SC (C) (C) C) c3cc (OCc4ccccn4) ccc23) cc1
Molecular Formula
C36H40N3NaO4S
Molecular Weight
633.78
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.

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