AM103

Additional information:
AM 103 is a potent and selective FLAP inhibitor, with an IC50 value of 4.2 nM.|Product information|CAS Number: 1147872-22-7|Molecular Weight: 632.77|Formula: C36H39N3NaO4S|Chemical Name: 3-[3-(tert-butylsulfanyl)-1-{[4-(6-methoxypyridin-3-yl)phenyl]methyl}-5-[(pyridin-2-yl)methoxy]-1H-indol-2-yl]-2,2-dimethylpropanoic acid sodium|Smiles: [Na].CC(C)(C)SC1C2=CC(=CC=C2N(CC2C=CC(=CC=2)C2=CN=C(C=C2)OC)C=1CC(C)(C)C(O)=O)OCC1=CC=CC=N1 |^1:0||InChiKey: VANSVYMYESBUFV-UHFFFAOYSA-N|InChi: InChI=1S/C36H39N3O4S.Na/c1-35(2,3)44-33-29-19-28(43-23-27-9-7-8-18-37-27)15-16-30(29)39(31(33)20-36(4,5)34(40)41)22-24-10-12-25(13-11-24)26-14-17-32(42-6)38-21-26;/h7-19,21H,20,22-23H2,1-6H3,(H,40,41);|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|AM 103 has an IC50 value of 349 nM in the human blood LTB4 inhibition assay. AM 103 has an excellent CYP profile against the 5 most common CYP isoforms with IC50 values greater than 30 μM for CYP2D6 and >50 μM for CYPs 3A4, 2C9 2C19, and 1A2. AM103 is a novel, potent, and selective FLAP inhibitor with IC50 values of 350, 113, and 117 nM against human, rat, and mouse whole-blood ionophore-stimulated LTB4 production, respectively.|In Vivo:|AM 103 has high bioavailability (64%), low clearance (2.9 mL/min/kg), low volume of distribution (0.41 L/kg), and a long i.v. half-life (5.2 h) in dogs. AM 103 (10 mg/kg q.i.d.) inhibits the increase in CysLTs and EPO by approximately 60%, and IL-5 levels are reduced to the concentrations obtained following saline treatment alone in mice.{{Spermidine} MedChemExpress|{Spermidine} Metabolic Enzyme/Protease|{Spermidine} Protocol|{Spermidine} Description|{Spermidine} custom synthesis|{Spermidine} Autophagy} AM103 (1 mg/kg, p.{{NRG-1 Protein, Human} medchemexpress|{NRG-1 Protein, Human} Biological Activity|{NRG-1 Protein, Human} In stock|{NRG-1 Protein, Human} custom synthesis|{NRG-1 Protein, Human} Cancer} o.PMID:24733396 ) displays >50% inhibition for up to 6 h with a calculated EC50 of appr 60 nM, in a rat ex vivo whole-blood calcium ionophore-induced LTB4 assay. AM 103 inhibits LTB4 and cysteinyl leukotriene (CysLT) production with ED50 values of 0.8 and 1 mg/kg, respectively, when rat lung is challenged in vivo with calcium ionophore. In this model, the EC50 derived from plasma AM103 is appr 330 nM for inhibition of both LTB4 and CysLT. In a model of chronic lung inflammation using ovalbumin-primed and challenged BALB/c mice, AM103 reduces the concentrations of eosinophil peroxidase, CysLTs, and interleukin-5 in the bronchoalveolar lavage fluid. Finally, AM 103 increases survival time in mice exposed to a lethal intravenous injection of platelet-activating factor.|Products are for research use only. Not for human use.|