| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 50mg | |||
| Other Sizes |
| Targets |
Atreleuton targets 5-lipoxygenase (5-LO) and 5-lipoxygenase-activating protein (FLAP), which are responsible for the biosynthesis of leukotrienes from arachidonic acid. It exhibits potent and selective inhibition of leukotriene formation with an IC50 of 23 nM in rat basophil leukemia cell lysates. By inhibiting FLAP, Atreleuton prevents the translocation and activation of 5-LO, thereby reducing the production of pro-inflammatory leukotrienes such as LTB4 and cysteinyl leukotrienes.
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| ln Vitro |
In vitro, Atreleuton potently inhibits 5-lipoxygenase activity and leukotriene formation. It exhibits an IC50 of 23 nM in rat basophil leukemia cell lysates. The compound selectively inhibits leukotriene biosynthesis without affecting other arachidonic acid metabolic pathways. Atreleuton has been shown to attenuate bronchoconstriction and pulmonary inflammation in rodent models, confirming its potent anti-inflammatory activity at the cellular level.
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| ln Vivo |
In vivo, Atreleuton has demonstrated efficacy in attenuating bronchoconstriction and pulmonary inflammation in rodent models. It has been studied extensively for its potential therapeutic applications in asthma, chronic obstructive pulmonary disease (COPD), and cardiovascular disease. The compound was investigated in clinical trials for cardiovascular disease, with VIA Pharmaceuticals meeting with the FDA to discuss Phase 3 outcome trials. Its oral bioavailability makes it suitable for chronic administration in research settings.
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| Enzyme Assay |
In vitro enzyme assays for Atreleuton typically measure its inhibition of 5-lipoxygenase activity using cell lysates or purified enzyme preparations. The enzyme is incubated with arachidonic acid substrate and the compound at varying concentrations, and the production of leukotrienes or their metabolites is quantified by HPLC or ELISA. The IC50 value is determined from dose-response curves. For FLAP inhibition, binding assays using radiolabeled FLAP ligands can be performed to assess the compound's ability to displace the ligand from the FLAP protein.
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| Cell Assay |
In vitro cell-based assays for Atreleuton are conducted using leukocyte or basophil cell lines stimulated with calcium ionophore or other agonists to induce leukotriene production. Cells are pre-incubated with Atreleuton at various concentrations, then stimulated, and the levels of leukotrienes (e.g., LTB4, LTD4) in the supernatant are measured by ELISA or LC-MS/MS. The IC50 for inhibition of leukotriene production is determined. Cytotoxicity is assessed using standard viability assays such as MTT or CellTiter-Glo to confirm that the observed inhibition is not due to cell death.
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| Animal Protocol |
In vivo animal experiments for Atreleuton have been conducted in rodent models of bronchoconstriction and pulmonary inflammation. In a typical study, rodents are administered Atreleuton orally or intraperitoneally prior to challenge with an antigen or a bronchoconstrictor agent. Airway resistance or inflammation markers are measured. The compound has been shown to attenuate bronchoconstriction and reduce pulmonary inflammation in a dose-dependent manner. Pharmacokinetic studies in animals have confirmed its oral bioavailability and favorable PK profile.
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| ADME/Pharmacokinetics |
Atreleuton has a molecular weight of 318.4 g/mol and a molecular formula of C16H15FN2O2S. It is soluble in DMSO but not in water. For storage, it is recommended to keep the powder at -20°C for up to 3 years or at 4°C for up to 2 years. In solvent, it can be stored at -80°C for 6 months or at -20°C for 1 month. The compound is stable at ambient temperature for a few days during shipping. It is orally bioavailable. Detailed pharmacokinetic parameters such as half-life and bioavailability have been characterized in preclinical and clinical studies.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for Atreleuton is not extensively detailed in standard product descriptions. As a compound that has been investigated in clinical trials, its safety profile has been evaluated in human studies. In preclinical studies, the compound was generally well-tolerated at therapeutic doses. Common side effects associated with 5-LO inhibitors may include gastrointestinal disturbances and liver enzyme elevations, though specific data for Atreleuton is not provided. As with all research chemicals, standard laboratory safety precautions should be followed when handling Atreleuton.
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| References | |
| Additional Infomation |
Atreleuton has been used in trials investigating the treatment of atherosclerosis and coronary artery disease.
Atreleuton (ABT-761, VIA-2291) is a research compound that has been investigated for the treatment of asthma, COPD, and cardiovascular disease. It is a selective, reversible, and orally bioavailable inhibitor of 5-lipoxygenase (5-LO) and FLAP. The compound was developed by Abbott and later by VIA Pharmaceuticals, which met with the FDA to discuss Phase 3 outcome trials for cardiovascular disease. Its mechanism of action involves inhibiting leukotriene biosynthesis, thereby reducing inflammation. Atreleuton is not approved for clinical use and is intended for research purposes only. |
| Exact Mass |
318.084
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|---|---|
| CAS # |
154355-76-7
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| Related CAS # |
154355-75-6 (racemic);154355-76-7;
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| PubChem CID |
3086671
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.37g/cm3
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| Boiling Point |
506.7ºC at 760mmHg
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| Flash Point |
260.2ºC
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| Vapour Pressure |
4.34E-11mmHg at 25°C
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| Index of Refraction |
1.652
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| LogP |
3.501
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
454
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@H](C#CC1=CC=C(S1)CC2=CC=C(C=C2)F)N(C(=O)N)O
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| InChi Key |
MMSNEKOTSJRTRI-LLVKDONJSA-N
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| InChi Code |
InChI=1S/C16H15FN2O2S/c1-11(19(21)16(18)20)2-7-14-8-9-15(22-14)10-12-3-5-13(17)6-4-12/h3-6,8-9,11,21H,10H2,1H3,(H2,18,20)/t11-/m1/s1
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| Chemical Name |
1-[(2R)-4-[5-[(4-fluorophenyl)methyl]thiophen-2-yl]but-3-yn-2-yl]-1-hydroxyurea
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| Synonyms |
ABT-761 Abbott-85761 VIA 2291 VIA-2291ABT 761Atreleuton VIA2291 A-85761
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00358826 | COMPLETEDWITH RESULTS | Drug: VIA-2291 Drug: Placebo |
Coronary Artery Disease | Tallikut Pharmaceuticals, Inc. | 2006-07 | Phase 2 |
| NCT00352417 | COMPLETEDWITH RESULTS | Drug: VIA-2291 Drug: Placebo |
Atherosclerosis | Tallikut Pharmaceuticals, Inc. | 2006-07 | Phase 2 |
| NCT00552188 | COMPLETEDWITH RESULTS | Drug: VIA-2291 Drug: Placebo |
Acute Coronary Syndrome | Tallikut Pharmaceuticals, Inc. | 2007-10 | Phase 2 |
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