| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
The primary target of AM-679 is the 5-lipoxygenase-activating protein (FLAP), which is an integral membrane protein that facilitates the transfer of arachidonic acid to 5-lipoxygenase (5-LO) for the synthesis of leukotrienes. By binding to FLAP, AM-679 inhibits the production of pro-inflammatory leukotrienes such as LTB4 and cysteinyl leukotrienes (CysLTs). This mechanism of action positions AM-679 as a key tool compound for studying the FLAP/5-LO pathway and its role in inflammatory and allergic diseases, as well as for evaluating the therapeutic potential of FLAP inhibition.
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| ln Vitro |
In an in vitro human FLAP membrane binding experiment, AM679 has an IC50 of 2 nM, indicating that it is a strong and selective FLAP inhibitor. The IC50 is 55 nM for both human blood and isolated ionophore-challenged mice as an inhibitor of LTB4 production. 154 nanometers [1]. With IC50 values of 2.2 nM/0.6 nM/154 nM for FLAP binding/hLA/hWB, respectively, AM679 is a strong and selective FLAP inhibitor[2].
AM-679 demonstrates potent in vitro activity with an IC50 of 2.2 nM in a human membrane FLAP binding assay. In human whole blood (hWB) assays, it exhibits an IC50 of 154 nM for inhibiting leukotriene production. The compound shows superior activity in cellular assays and has an improved cytochrome P450 (CYP) inhibition profile compared to other FLAP inhibitors, with IC50 values of 16.7 μM for CYP3A4, 3.7 μM for CYP2C9, and >30 μM for CYP2D6. Additionally, it shows no time-dependent inhibition or induction of CYP3A4, indicating a favorable drug-drug interaction potential. |
| ln Vivo |
In mouse bronchoalveolar lavage challenge models and human blood, AM679 exhibits strong inhibitory effects on leukotrienes [2].
In rodent bronchoalveolar lavage (BAL) models, AM-679 demonstrates strong in vivo inhibition of leukotriene production following oral administration. At a dose of 10 mg/kg administered orally 4 hours before ionophore challenge, AM-679 significantly reduces LTB4 levels by 98% and CysLT levels by 87% in the BAL fluid. This potent in vivo efficacy confirms its ability to engage the FLAP target and suppress the downstream leukotriene pathway in a relevant animal model of pulmonary inflammation, supporting its utility for in vivo pharmacological studies. |
| Enzyme Assay |
The in vitro enzyme/receptor binding assay for AM-679 typically involves a competition binding assay using human membrane preparations expressing FLAP. Radiolabeled ligands, such as [³H]-labeled FLAP inhibitors, are incubated with varying concentrations of AM-679 and the membrane protein in a suitable buffer. After incubation to reach equilibrium, the bound and free radioligands are separated, typically by filtration or centrifugation, and the radioactivity is measured to calculate the IC50 value. The assay determines the compound's affinity for FLAP by measuring its ability to displace the radiolabeled probe, with AM-679 showing a binding IC50 of 2.2 nM.
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| Cell Assay |
Cellular activity of AM-679 is assessed using human whole blood (hWB) assays to measure its inhibition of leukotriene production. In this assay, human blood is incubated with various concentrations of the compound, typically pre-incubated for a specific time, and then stimulated with a calcium ionophore to trigger the leukotriene synthesis pathway. After stimulation, the levels of leukotriene B4 (LTB4) and cysteinyl leukotrienes (CysLTs) in the blood are quantified using ELISA or LC-MS/MS. The compound's potency is determined by calculating the IC50 value for inhibiting leukotriene production, which for AM-679 is 154 nM in hWB assays.
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| Animal Protocol |
The primary in vivo model for evaluating AM-679 is the rodent bronchoalveolar lavage (BAL) model. In this model, rodents (typically rats or mice) are administered AM-679 orally at a specified dose (e.g., 10 mg/kg). After a predetermined time (e.g., 4 hours), the animals are challenged with a calcium ionophore, often administered intratracheally or intravenously, to stimulate leukotriene production in the lungs. Following the challenge, BAL fluid is collected, and the levels of LTB4 and CysLTs are measured using immunoassays to assess the compound's in vivo efficacy.
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| ADME/Pharmacokinetics |
AM-679 displays favorable pharmacokinetic properties suitable for oral administration. It shows strong in vivo activity in rodent models after oral dosing, indicating good oral bioavailability. The compound is soluble in DMSO at ≥80 mg/mL and can be formulated for in vivo administration using a vehicle such as 10% DMSO in 90% corn oil. Its improved CYP inhibition profile suggests a lower risk for drug-drug interactions compared to other compounds in its class. However, detailed pharmacokinetic parameters such as half-life, clearance, and volume of distribution are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
Available data indicate that AM-679 has an improved safety profile relative to other FLAP inhibitors, as it displays reduced cytochrome P450 inhibition characteristics. Specifically, it shows no time-dependent inhibition or induction of CYP3A4, which are common causes of drug-drug interactions and toxicity. The compound has IC50 values of >30 μM against CYP2D6, indicating low potential for inhibiting this major drug-metabolizing enzyme. However, comprehensive toxicology data, including acute and chronic toxicity studies, genotoxicity, and carcinogenicity assessments, are not publicly available for this research compound.
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| References |
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| Additional Infomation |
AM-679 is a research-grade compound exclusively intended for preclinical investigations and is not approved for clinical use. Its primary application is as a pharmacological tool to study the role of FLAP and leukotrienes in inflammatory diseases. The compound's favorable CYP inhibition profile and potent in vivo efficacy make it a valuable asset for drug discovery programs targeting the leukotriene pathway. Researchers must be aware that "AM-679" also refers to a cannabinoid receptor agonist with a distinct CAS number (335160-91-3), and careful verification of the compound's identity is essential for experimental reproducibility.
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| Molecular Formula |
C20H20INO
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| Molecular Weight |
417.28
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| Exact Mass |
692.303
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| CAS # |
1206880-66-1
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| PubChem CID |
44627267
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| Appearance |
Off-white to pink solid powder
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| LogP |
8.12
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
50
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| Complexity |
1150
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(=O)N1[C@@H](CC2=CC=CC=C21)COC3=CC4=C(C=C3)N(C(=C4SC(C)(C)C)CC(C)(C)C(=O)O)CC5=CC=C(C=C5)C6=NC=C(C=N6)OC
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| InChi Key |
VYXWHVDEWWHDLH-LJAQVGFWSA-N
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| InChi Code |
InChI=1S/C40H44N4O5S/c1-25(45)44-29(18-28-10-8-9-11-33(28)44)24-49-30-16-17-34-32(19-30)36(50-39(2,3)4)35(20-40(5,6)38(46)47)43(34)23-26-12-14-27(15-13-26)37-41-21-31(48-7)22-42-37/h8-17,19,21-22,29H,18,20,23-24H2,1-7H3,(H,46,47)/t29-/m0/s1
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| Chemical Name |
1-Pentyl-3-(2-iodobenzoyl)indole
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| Synonyms |
AM-679 AM679AM 679 SCHEMBL503239 65KJ8P7M9DUNII-65KJ8P7M9D CHEMBL595092
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~144.33 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.75 mg/mL (3.97 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (3.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3965 mL | 11.9824 mL | 23.9647 mL | |
| 5 mM | 0.4793 mL | 2.3965 mL | 4.7929 mL | |
| 10 mM | 0.2396 mL | 1.1982 mL | 2.3965 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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