| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
ALOX15-IN-1 targets the 15-lipoxygenase enzymes ALOX15, which are key enzymes in polyunsaturated fatty acid (PUFA) metabolism. It inhibits the linoleate oxygenase activity of rabbit and human ALOX15 orthologs. The compound exhibits differential potency depending on the substrate, showing high potency for linoleic acid (LA) as a substrate and weaker, yet specific, activity with arachidonic acid (AA). This allows for the dissection of substrate-specific functions of ALOX15.
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| ln Vitro |
In vitro, ALOX15-IN-1 potently inhibits the rabbit ALOX15-catalyzed oxygenation of linoleic acid (LA) with an IC50 of 0.04 microM. It also inhibits the human ALOX15-catalyzed oxygenation of LA with an IC50 of 2.06 microM, demonstrating species and substrate selectivity. The compound is specific for the linoleate oxygenase activity of ALOX15. These activities make it a potent inhibitor for probing the function of ALOX15 in various biological systems.
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| ln Vivo |
In vivo activity data for ALOX15-IN-1 is not extensively published. As a potent and specific inhibitor of ALOX15, it has the potential to be used in animal models of diseases where this enzyme is implicated, such as inflammation, asthma, and cancer. Based on its in vitro potency, researchers would typically administer it via intraperitoneal or oral routes to study the in vivo effects of ALOX15 inhibition. Formal in vivo efficacy studies would need to be conducted.
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| Enzyme Assay |
To determine ALOX15-IN-1's inhibitory effect, an in vitro enzyme assay is performed. Recombinant rabbit or human ALOX15 protein is incubated in reaction buffer with varying concentrations of ALOX15-IN-1 (e.g., 0.01-100 microM). The reaction is initiated by the addition of the substrate, either linoleic acid (LA) or arachidonic acid (AA). After incubation at room temperature for a set time (e.g., 10-30 minutes), the reaction is stopped. The oxygenated products (hydroperoxyoctadecadienoic acid from LA) are extracted and quantified by HPLC or UV spectrophotometry.
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| Cell Assay |
ALOX15-IN-1 is a research tool and is not a therapeutic. For cell-based assays, macrophages or other relevant cell lines expressing ALOX15 are treated with ALOX15-IN-1 at concentrations around its IC50 values. After treatment, cells are stimulated with a calcium ionophore or other activators to trigger the arachidonic acid cascade. The levels of 15-HETE (the product of ALOX15 acting on arachidonic acid) in the cell supernatant are measured by ELISA or LC-MS/MS to assess the compound's cell-based efficacy. Cytotoxicity is assessed via an LDH release or MTT assay.
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| Animal Protocol |
In vivo procedures for ALOX15-IN-1 are not well-documented in the public literature. As with other lipoxygenase inhibitors, it would be formulated in a suitable vehicle for oral or intraperitoneal administration. For a typical rodent study, animals would be pre-treated with the compound, then challenged with an inflammatory agent (e.g., carrageenan or LPS). Tissue or blood samples would be collected to measure oxylipin levels and inflammatory markers via LC-MS/MS or ELISA to determine the compound's in vivo efficacy.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for ALOX15-IN-1 is not publicly available. The compound has a molecular weight of 473.59 g/mol and a predicted LogP of 6.5, suggesting high lipophilicity. This may result in poor aqueous solubility and potentially high protein binding. For in vivo studies, it is recommended to formulate in DMSO with co-solvents like PEG300, Tween 80, or cyclodextrins to enhance solubility. Researchers should conduct pilot PK studies to determine key parameters like half-life and bioavailability.
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| Toxicity/Toxicokinetics |
Published toxicological data for ALOX15-IN-1 is limited to its in vitro selectivity profile. It is a specific ALOX15 inhibitor, which may minimize off-target effects. In cell-based assays at concentrations up to its IC50 (2.06 microM for human ALOX15/AA), no significant toxicity is reported. As with any novel chemical entity, thorough safety and toxicity studies would be required before any advancement. The compound is for research use only.
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| References | |
| Additional Infomation |
ALOX15-IN-1 is a research-grade compound and is not approved for clinical use. It is primarily a tool for studying the biology of the ALOX15 enzyme, particularly its linoleate oxygenase activity. The differential potency between the rabbit and human enzymes and between substrates is a key feature for mechanistic studies. The compound should be stored as a powder at -20degC, protected from light and moisture, and is soluble in DMSO. For research use only.
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| Molecular Formula |
C24H31N3O5S
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|---|---|
| Molecular Weight |
473.585045099258
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| Exact Mass |
473.198
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| CAS # |
2764818-24-6
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| PubChem CID |
163322029
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
6.5
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
33
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| Complexity |
699
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCCCCOC(=O)NS(=O)(=O)NC1=C(C=CC(=C1)C2=CC3=CC=CC=C3N2)OC
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| InChi Key |
OMEJTIUQCWVECC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H31N3O5S/c1-3-4-5-6-7-10-15-32-24(28)27-33(29,30)26-22-17-19(13-14-23(22)31-2)21-16-18-11-8-9-12-20(18)25-21/h8-9,11-14,16-17,25-26H,3-7,10,15H2,1-2H3,(H,27,28)
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| Chemical Name |
octyl N-[[5-(1H-indol-2-yl)-2-methoxyphenyl]sulfamoyl]carbamate
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1115 mL | 10.5577 mL | 21.1153 mL | |
| 5 mM | 0.4223 mL | 2.1115 mL | 4.2231 mL | |
| 10 mM | 0.2112 mL | 1.0558 mL | 2.1115 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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