| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
| Targets |
12R-lipoxygenase (12R-LOX)[1]
12R-LOX-IN-2 targets 12R-lipoxygenase (12R-LOX), an enzyme that plays a role in epidermal lipid processing and inflammatory responses. By inhibiting this enzyme, the compound modulates lipid metabolism and reduces keratinocyte hyperproliferation. |
|---|---|
| ln Vitro |
In vitro, 12R-LOX-IN-2 inhibits imiquimod (IMQ)-induced hyperproliferation of psoriatic keratinocytes and suppresses colony formation. It also decreases the protein level of Ki67 (a proliferation marker) and the mRNA expression of IL-17A (a pro-inflammatory cytokine) in IMQ-induced cells.
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| ln Vivo |
Specific in vivo activity data for 12R-LOX-IN-2 are not detailed in the available literature. However, its ability to inhibit IMQ-induced hyperproliferation of psoriatic keratinocytes in vitro suggests potential for in vivo efficacy in animal models of psoriasis, such as the IMQ-induced mouse model of psoriasis.
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| Enzyme Assay |
Non-cellular enzyme assays for 12R-LOX-IN-2 involve measuring its inhibitory activity against purified 12R-LOX enzyme. The compound is incubated with the enzyme and a substrate, and the inhibition of lipoxygenase activity is quantified to determine its potency as an inhibitor.
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| Cell Assay |
In vitro cellular assays for 12R-LOX-IN-2 are performed using psoriatic keratinocytes induced with imiquimod (IMQ). The compound's ability to inhibit hyperproliferation is assessed by measuring cell viability and colony formation. The expression of proliferation markers like Ki67 and inflammatory cytokines like IL-17A are also measured.
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| Animal Protocol |
In vivo animal experiments for 12R-LOX-IN-2 would likely involve the IMQ-induced mouse model of psoriasis. The compound would be administered topically or systemically, and its effects on skin inflammation, epidermal thickness, and the expression of inflammatory markers would be evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties for 12R-LOX-IN-2 are not detailed in the available literature. As a small molecule inhibitor, its PK profile would be important for determining its suitability for topical or systemic administration in the treatment of skin diseases.
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| Toxicity/Toxicokinetics |
Toxicological data for 12R-LOX-IN-2 are not provided in the available sources. As a research compound, its safety profile has not been extensively characterized. It is intended for research use only and not for human consumption.
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| References | |
| Additional Infomation |
12R-LOX-IN-2 has a molecular weight of 271.31 and a molecular formula of C19H13NO. Its CAS number is 3026677-37-9. The compound appears as a yellow solid and is soluble in DMSO. It should be stored as a powder at -20°C. It is supplied for research purposes only.
|
| Molecular Formula |
C19H13NO
|
|---|---|
| Molecular Weight |
271.31
|
| Exact Mass |
271.1
|
| CAS # |
3026677-37-9
|
| PubChem CID |
168679704
|
| Appearance |
Off-white to yellow solid powder
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| Density |
1.264±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
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| Boiling Point |
469.5±30.0 °C(predicted)
|
| LogP |
0
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
21
|
| Complexity |
357
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC=C2C(=C1)C=CC(=N2)C3=CC=C(C4=CC=CC=C43)O
|
| InChi Key |
PLATVCRZPNTREE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H13NO/c21-19-12-10-15(14-6-2-3-7-16(14)19)18-11-9-13-5-1-4-8-17(13)20-18/h1-12,21H
|
| Chemical Name |
4-quinolin-2-ylnaphthalen-1-ol
|
| 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 | 3.6858 mL | 18.4291 mL | 36.8582 mL | |
| 5 mM | 0.7372 mL | 3.6858 mL | 7.3716 mL | |
| 10 mM | 0.3686 mL | 1.8429 mL | 3.6858 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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