AM103
Based on 1 Customer Validation
AM 103 is a potent and selective FLAP inhibitor, with an IC50 value of 4.2 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.59%
- No. CAS: 1147872-22-7
- Fòrmula: C36H38N3NaO4S
- Peso molecular:631.76
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Almacenamiento:
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)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
IC50: 4.2 nM (FLAP)[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1147872-22-7
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Appearance Solid
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Peso molecular 631.76
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Fòrmula C36H38N3NaO4S
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Color Off-white to light yellow
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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)
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Hutchinson JH, et al. 5-lipoxygenase-activating protein inhibitors: development of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103). J Med Chem. 2009 Oct 8;52(19):5803 [Content Brief]
[2]. Lorrain DS, et al. Pharmacological characterization of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103), a novel selective 5-lipoxygenase-activating protein inhibitor [Content Brief]
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 |
AM103 Related Classifications
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