| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
Lonapalene targets 5-lipoxygenase (5-LO), the key enzyme in the biosynthesis of leukotrienes from arachidonic acid. By inhibiting 5-LO, it blocks the production of leukotrienes, including leukotriene B4, which are important mediators of inflammation in psoriasis and other inflammatory conditions.
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|---|---|
| ln Vitro |
Leukotriene B4 is a significant mediator of the pathophysiology of psoriasis, and lonsapalene (RS4317) is helpful in treating this condition [1].
Lonapalene demonstrates 5-lipoxygenase inhibitory activity in vitro. It blocks skin inflammation through topical application. The compound is used to study the role of leukotriene B4 as a mediator in psoriasis pathology. In vitro activity is confirmed through enzyme inhibition assays using purified 5-LO. |
| ln Vivo |
Lonapalene has topical anti-psoriasis efficacy in vivo. It is topically effective for treating psoriasis. The compound blocks skin inflammation through topical application. Clinical pharmacology studies have been conducted to assess its efficacy and safety.
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| Enzyme Assay |
Non-cell-based enzyme assays for Lonapalene use purified 5-lipoxygenase enzyme. The compound is incubated with the enzyme, arachidonic acid substrate, and cofactors at varying concentrations. 5-LO activity is measured by quantifying leukotriene production using techniques such as HPLC, ELISA, or mass spectrometry. IC50 values for enzyme inhibition are determined. Assays are performed in buffered solutions at physiological pH.
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| Cell Assay |
Cellular assays for Lonapalene utilize leukocytes or other 5-LO-expressing cells stimulated with calcium ionophore or other activators to induce leukotriene production. Cells are treated with the compound at various concentrations, and leukotriene B4 or other leukotriene levels in the supernatant are measured by ELISA. Cell viability is assessed to ensure specificity of the inhibitory effect.
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| Animal Protocol |
In vivo animal models for Lonapalene include standard models of skin inflammation such as the mouse ear edema model or psoriasis-like models. The compound is applied topically at various concentrations. Inflammation is assessed by measuring ear thickness, histopathological analysis, and inflammatory mediator levels in skin tissue. Clinical studies in psoriasis patients have also been conducted.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Lonapalene include molecular weight of 338.74 g/mol and molecular formula as a naphthalene derivative. The compound is designed for topical administration, with percutaneous absorption and metabolism studied. As a topical agent, systemic exposure is expected to be limited. Detailed PK parameters are not extensively reported.
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| Toxicity/Toxicokinetics |
Lonapalene is a topical agent with anti-inflammatory activity. It was initially developed by F. Hoffmann-La Roche Ltd. As a 5-LO inhibitor, it blocks leukotriene production. Detailed toxicity data are not extensively reported, but topical agents generally have a favorable safety profile compared to systemic drugs. Clinical studies have been conducted to assess safety and efficacy.
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| References | |
| Additional Infomation |
Lonapalene is an organochlorine compound, belonging to the naphthalene family of compounds.
Lonapalene is also known as RS4317 and RS-43179. It has CAS number 91431-42-4. The compound is a 5-lipoxygenase inhibitor with anti-psoriasis efficacy. It was developed for the treatment of psoriasis and other skin-related conditions. It is supplied as a research compound. |
| Molecular Formula |
C16H15CLO6
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|---|---|
| Molecular Weight |
338.74
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| Exact Mass |
338.056
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| CAS # |
91431-42-4
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| PubChem CID |
56237
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| Appearance |
White to light yellow solid powder
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| Density |
1.309g/cm3
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| Boiling Point |
424.9ºC at 760mmHg
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| Flash Point |
159.3ºC
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| Index of Refraction |
1.571
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| LogP |
3.361
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
23
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| Complexity |
442
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IFWMVQUGSGWCRP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H15ClO6/c1-8(18)22-13-11-6-5-10(17)7-12(11)14(23-9(2)19)16(21-4)15(13)20-3/h5-7H,1-4H3
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| Chemical Name |
(4-acetyloxy-6-chloro-2,3-dimethoxynaphthalen-1-yl) acetate
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| Synonyms |
RS 43179; RS-43179; Lonapalene
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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 (~295.21 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 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: ≥ 2.5 mg/mL (7.38 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 25.0 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 | 2.9521 mL | 14.7606 mL | 29.5212 mL | |
| 5 mM | 0.5904 mL | 2.9521 mL | 5.9042 mL | |
| 10 mM | 0.2952 mL | 1.4761 mL | 2.9521 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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