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AM103

CAT: 0013-GTR19216977-03Size: 1 gDry Ice: NoHazardous: No
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CAT#:0013-GTR19216977-03Size:1 g
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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.

Chemical Information

AM-103

AM103 is a novel inhibitor of 5-lipoxygenase-activiting protein (FLAP) that has demonstrated potential to treat asthma and cardiovascular disease by preventing the synthesis of LT, which triggers inflammation. It is being developed by Amira.

CAS Number1147872-22-7
PubChem CID59248882
IUPAC Namesodium 3-[3-tert-butylsulfanyl-1-[[4-(6-methoxy-3-pyridinyl)phenyl]methyl]-5-(pyridin-2-ylmethoxy)indol-2-yl]-2,2-dimethylpropanoate
Molecular FormulaC36H38N3NaO4S
Molecular Weight631.8
Topological Polar Surface Area115
Hydrogen Bond Donor Count0
Hydrogen Bond Acceptor Count7
Rotatable Bond Count12
Heavy Atom Count45
Formal Charge0
Complexity926
SMILES
CC(C)(C)SC1=C(N(C2=C1C=C(C=C2)OCC3=CC=CC=N3)CC4=CC=C(C=C4)C5=CN=C(C=C5)OC)CC(C)(C)C(=O)[O-].[Na+]
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);/q;+1/p-1
InChIKey
NJJMCCVPHCNMPB-UHFFFAOYSA-M
Chemical Structure
2D Structure
2D structure of AM-103
CAS: 1147872-22-7
CID: 59248882
Formula: C36H38N3NaO4S
MW: 631.8
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight631.8
Hydrogen Bond Donor Count0
Hydrogen Bond Acceptor Count7
Rotatable Bond Count12
Exact Mass631.24807216
Monoisotopic Mass631.24807216
Topological Polar Surface Area115 Ų
Heavy Atom Count45
Formal Charge0
Complexity926
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count2
Compound Is CanonicalizedYes

Alternative Products

CatalogName
MBS5766046AM103
HY-14162AM103 (free acid)

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