AM103

SKU: orb1310001

Description

AM103 is a potent and selective FLAP inhibitor with an IC50 of 4.2 nM. This small molecule is a valuable research tool for investigating leukotriene biosynthesis in cellular assays and animal models of inflammation.

Research Area

Immunology & Inflammation

Key Properties

• CAS Number: 1147872-22-7
• MW: 631.76
• Purity: 99.75%
• Formula: C₃₆H₃₈N₃NaO₄S
• SMILES: [Na+].COc1ccc(cn1)-c1ccc(Cn2c(CC(C)(C)C([O-])=O)c(SC(C)(C)C)c3cc(OCc4ccccn4)ccc23)cc1
• Target: FLAP
• Solubility: 10% DMSO+90% Corn Oil:5 mg/mL (7.91 mM);DMSO:180 mg/mL (284.92 mM)

Bioactivity

• Target IC50:
  FLAP:4.2 nM
• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AM103, AM-103, AM 103, FLAP

Compound Identifiers

PubChem CID

59248882