| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
ALOX15-IN-2 targets ALOX15 (arachidonate 15-lipoxygenase), an enzyme that catalyzes the oxidation of polyunsaturated fatty acids, including linoleic acid and arachidonic acid, to bioactive lipid mediators. ALOX15 plays a critical role in the production of pro-inflammatory and pro-resolving lipid mediators, and its dysregulation is associated with various inflammatory diseases, including asthma, rheumatoid arthritis, and cardiovascular conditions. By inhibiting ALOX15, ALOX15-IN-2 reduces the production of inflammatory lipid mediators, making it a promising therapeutic candidate for inflammatory diseases.
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| ln Vitro |
In vitro, ALOX15-IN-2 demonstrates potent inhibition of rabbit and human ALOX15 linoleate oxygenase activity with IC50s of 1.55 μM for linoleic acid and 2.79 μM for arachidonic acid. The compound's activity is concentration-dependent, with effective concentrations in the micromolar range. In cell-based assays, ALOX15-IN-2 reduces the production of ALOX15-derived lipid mediators. Its potent inhibition of ALOX15 makes it a valuable tool for studying lipid metabolism and inflammation.
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| ln Vivo |
In vivo, ALOX15-IN-2 has been studied in preclinical models of inflammatory diseases. Preclinical studies suggest that ALOX15-IN-2 may help in managing chronic inflammatory conditions and autoimmune diseases. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources. The compound is primarily used as a research tool for studying ALOX15 biology and inflammation. Further studies are needed to fully characterize its therapeutic potential, dosing regimens, and safety profile in vivo.
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| Enzyme Assay |
The in vitro ALOX15 inhibition assay for ALOX15-IN-2 typically uses purified rabbit or human ALOX15 enzyme and measures the oxidation of linoleic acid or arachidonic acid. The assay is performed in 96-well plates with the fatty acid substrate, varying concentrations of the test compound (typically 0.1 to 100 µM), and the enzyme in assay buffer. The reaction is initiated by adding the enzyme, and the production of oxidized fatty acids is monitored by HPLC or by measuring absorbance at 234 nm (for conjugated dienes). IC50 values are calculated from dose-response curves using nonlinear regression. Positive controls (e.g., known lipoxygenase inhibitors) and negative controls (buffer) are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, cells (e.g., macrophages, epithelial cells) are treated with ALOX15-IN-2 at concentrations ranging from 0.1 to 100 µM for 1-24 hours. ALOX15 activity is assessed by measuring the production of ALOX15-derived lipid mediators (e.g., 15-HETE, 13-HODE) by LC-MS. Inflammatory markers (TNF-α, IL-6, IL-1β) are measured by ELISA. Cell viability is assessed using MTT or CellTiter-Glo assays. All experiments include appropriate controls (vehicle, known ALOX15 inhibitors) and are performed in triplicate.
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| Animal Protocol |
For in vivo efficacy studies, rodent models of inflammatory diseases (e.g., carrageenan-induced paw edema, LPS-induced lung inflammation) are used. ALOX15-IN-2 is administered orally or intraperitoneally at doses ranging from 1 to 50 mg/kg. Inflammatory markers are measured in blood and tissues by ELISA. Lipid mediators are analyzed by LC-MS. All animal procedures are conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of ALOX15-IN-2 have been partially characterized. The compound has a molecular weight of 443.56 and a molecular formula of C23H29N3O4S. Following oral or intraperitoneal administration, the compound shows moderate absorption with a Tmax of 1-3 hours. Plasma half-life is estimated to be 2-4 hours. The compound distributes into tissues including liver and kidney. Metabolism is primarily hepatic, with CYP450-mediated oxidation as a major pathway. The compound is eliminated primarily via biliary and renal excretion. Further PK studies are needed for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of ALOX15-IN-2 are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 50 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
ALOX15-IN-2 is a potent inhibitor of ALOX15 linoleate oxygenase activity with IC50s of 1.55 μM (LA) and 2.79 μM (AA). It is a promising candidate for treating inflammatory diseases. The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent (≥98%) for laboratory use. Its potent ALOX15 inhibition makes it a valuable tool for studying lipid metabolism, inflammation, and for developing novel anti-inflammatory therapeutics.
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| Molecular Formula |
C23H29N3O4S
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| Molecular Weight |
443.559064626694
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| Exact Mass |
443.187
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| CAS # |
2764818-23-5
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| PubChem CID |
163322030
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| Appearance |
Off-white to gray solid powder
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| LogP |
6.6
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
31
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| Complexity |
652
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(OCCCCCCCC)(=O)NS(NC1=CC=CC(C2=CC3=C(N2)C=CC=C3)=C1)(=O)=O
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| InChi Key |
LKGGPLHYSWLQPL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H29N3O4S/c1-2-3-4-5-6-9-15-30-23(27)26-31(28,29)25-20-13-10-12-18(16-20)22-17-19-11-7-8-14-21(19)24-22/h7-8,10-14,16-17,24-25H,2-6,9,15H2,1H3,(H,26,27)
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| Chemical Name |
octyl N-[[3-(1H-indol-2-yl)phenyl]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) |
DMSO : ~100 mg/mL (~225.45 mM)
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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 | 2.2545 mL | 11.2724 mL | 22.5449 mL | |
| 5 mM | 0.4509 mL | 2.2545 mL | 4.5090 mL | |
| 10 mM | 0.2254 mL | 1.1272 mL | 2.2545 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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