2. Immunology/Inflammation
  3. FLAP
  4. AM103

AM 103 is a potent and selective FLAP inhibitor, with an IC50 value of 4.2 nM.

For research use only. We do not sell to patients.

AM103 Chemical Structure

AM103 Chemical Structure

CAS No. : 1147872-22-7

Size Price Stock Quantity
1 mg USD 176 In-stock
5 mg USD 440 In-stock
10 mg USD 660 In-stock
25 mg USD 1188 In-stock
50 mg USD 1663 In-stock
100 mg USD 2300 In-stock
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AM103 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

AM 103 is a potent and selective FLAP inhibitor, with an IC50 value of 4.2 nM.

IC50 & Target

IC50: 4.2 nM (FLAP)[1]
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[1]. 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[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AM103 Related Antibodies
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[1]. AM103 (1 mg/kg, p.o.) 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[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

631.76

Formula

C36H38N3NaO4S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(O[Na])C(C)(C)CC(N1CC2=CC=C(C3=CC=C(OC)N=C3)C=C2)=C(SC(C)(C)C)C4=C1C=CC(OCC5=NC=CC=C5)=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (316.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5829 mL 7.9144 mL 15.8288 mL
5 mM 0.3166 mL 1.5829 mL 3.1658 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 5 mg/mL (7.91 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (7.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Kinase Assay
[1]

Packed human polymorphonuclear cell pellets (1.8×109 cells) are resuspended, lysed, and 75,000g membranes. The 75,000g pelleted membranes are resuspended in a Tris buffer (50 mM Tris HCl, pH 7.4, 1 mM EDTA, 1 mM DTT, and 30% glycerol) to yield a protein concentration of appr 4 mg/mL. Then, 2.5 μg of membrane protein per well is added to 96-well deep well plates containing Tris-Tween buffer (100 mM Tris HCl, pH 7.4, 100 mM NaCl, 1 mM EDTA, 0.5 mM DTT, 5% glycerol, and 0.05% Tween-20) and appr 30,000 cpm of [3H]-3-[5-(pyrid-2-ylmethoxy)-3-tert-butylthio-1-benzyl-indol-2-yl]-2,2-dimethylpropionic acid and test compound in a total volume of 100 μL and incubated for 60 min at room temperature. The reactions are then harvested onto GF/B filter plates using a Brandel 96-tip harvester and washed 3× with 1 mL of ice-cold Tris-Tween buffer. The filter plates are dried, the bottoms sealed, and 100 μL of scintillant added. The plates are incubated for 1 h before reading on Perkin-Elmer TopCount. Specific binding is defined as total radioactive binding minus nonspecific binding in the presence of 10 μM MK886. IC50 values are determined using Graphpad prism analysis of drug titration curves.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Compounds are administered intravenously (i.v.) (2 mg/kg) to two or three male rats (fasted overnight) as a solution in PEG400/ethanol/water (40/10/50, v/v/v) via a bolus injection into the jugular vein (2 mg/mL; 1 mL/kg) and orally (p.o.) (10 mg/kg) to two or three male rats as a suspension in 0.5% methylcellulose via an oral gavage to the stomach (3.33 mg/mL; 3 mL/kg). Blood samples (approximately 300 μL) are taken from each rat via the jugular vein cannula at time intervals up to 24 h postdose (8−9 samples per animal). After each sample, the cannula is flushed with an equivalent volume of heparinized saline (0.1 mL at 40 units/mL). Plasma samples, prepared by centrifugation of whole blood, are stored frozen (−80°C) prior to analysis.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5829 mL 7.9144 mL 15.8288 mL 39.5720 mL
5 mM 0.3166 mL 1.5829 mL 3.1658 mL 7.9144 mL
10 mM 0.1583 mL 0.7914 mL 1.5829 mL 3.9572 mL
15 mM 0.1055 mL 0.5276 mL 1.0553 mL 2.6381 mL
20 mM 0.0791 mL 0.3957 mL 0.7914 mL 1.9786 mL
25 mM 0.0633 mL 0.3166 mL 0.6332 mL 1.5829 mL
30 mM 0.0528 mL 0.2638 mL 0.5276 mL 1.3191 mL
40 mM 0.0396 mL 0.1979 mL 0.3957 mL 0.9893 mL
50 mM 0.0317 mL 0.1583 mL 0.3166 mL 0.7914 mL
60 mM 0.0264 mL 0.1319 mL 0.2638 mL 0.6595 mL
80 mM 0.0198 mL 0.0989 mL 0.1979 mL 0.4946 mL
100 mM 0.0158 mL 0.0791 mL 0.1583 mL 0.3957 mL
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AM103 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AM1031147872-22-7AM 103AM-103FLAP5-lipoxygenase-activating protein5-LO activating proteinInhibitorinhibitorinhibit

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