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| 5mg |
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| 50mg |
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| Targets |
Frentizole targets the Aβ-ABAD interaction. ABAD is an enzyme that binds to amyloid beta (Aβ) peptide, and this interaction is thought to contribute to the neurotoxicity in Alzheimer's disease. By inhibiting this interaction, frentizole may have neuroprotective effects. It also targets tubulin, inhibiting microtubule polymerization and exerting antitumor effects. Its immunosuppressive effects are mediated through other mechanisms.
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| ln Vitro |
When combined with mitogens, frentizole (500 ng/mL, 48 h) potently inhibits the incorporation of thymidine into DNA in lymphocyte cultures. It also strongly inhibits lymphocytes that are retrieved from the peritoneal cavity of mice in a way that is dependent on dose. In cells, 58% of the cells responded to concanavalin A [1]. The effective suppression of uridine incorporation by fermizole (62.5 ng/mL) is not reliant on the specific phytochemical employed [1].
In vitro, frentizole is an inhibitor of the Aβ-ABAD interaction with an IC50 of 200 μM. It has immunosuppressive activity. It displays antitumor activity via tubulin inhibition. Its antiviral properties have also been demonstrated. Its effects on cell proliferation and immune cell function have been characterized. |
| ln Vivo |
For a period of 52 weeks, lentizole (8.2 or 79.9 mg/kg/day) can prolong the lives of NZB/NZW mice [2].
In vivo, frentizole is used clinically as an immunosuppressive agent for rheumatoid arthritis and systemic lupus erythematosus. Its immunosuppressive effects help to reduce inflammation and autoimmunity. Its potential as an antitumor agent is being investigated. |
| Enzyme Assay |
In vitro enzyme assays for frentizole measure its inhibition of the Aβ-ABAD interaction. The compound is incubated with ABAD and Aβ peptide, and the interaction is measured by fluorescence polarization or other methods. Its inhibition of tubulin polymerization can be assessed by spectrophotometry.
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| Cell Assay |
In vitro cell-based assays for frentizole involve treating cells with the compound and measuring its effects on cell viability, proliferation, and immune function. Its effects on microtubule dynamics are assessed by immunofluorescence. Its immunosuppressive effects are assessed by measuring cytokine production and lymphocyte proliferation.
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| Animal Protocol |
Animal/Disease Models: NZB/NZW mice [2]
Doses: Young mice 8.2 or 79.9 mg/kg/day Route of Administration: In animal breeding; 52 weeks Experimental Results: demonstrated that the average life span of untreated young mice was 38 weeks, The low-dose group lived an average of about 38 weeks, and the high-dose group lived Dramatically longer, with an average lifespan of about 61 weeks. The white blood cell counts were Dramatically suppressed compared with the average peripheral blood leukocyte count of 4160 in control mice, 3217 in low-dose treated mice, and 3450 in high-dose treated mice. Terminal neutrophil counts were Dramatically increased in young mice treated with both low and high doses compared with controls. In vivo animal experiments for frentizole have been conducted in models of autoimmune diseases and cancer. Animals are treated with the compound, and its effects on inflammation and tumor growth are assessed. Its immunosuppressive and antitumor activities have been demonstrated in these models. |
| ADME/Pharmacokinetics |
Frentizole has a molecular weight of 299.35 and a molecular formula of C15H13N3O2S. Its exact mass is 299.0728. It is a solid compound typically stored under recommended conditions.
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| Toxicity/Toxicokinetics |
Frentizole is an FDA-approved immunosuppressant. Its safety profile has been established in clinical use. It is generally well-tolerated. It is a research compound and is not intended for human use without proper authorization.
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| References |
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| Additional Infomation |
Frentizole is an immunosuppressive agent and an inhibitor of the Aβ-ABAD interaction. It is used clinically in rheumatoid arthritis and systemic lupus erythematosus. It has antitumor activity via tubulin inhibition. It is a benzothiazole derivative.
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| Molecular Formula |
C15H13N3O2S
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| Molecular Weight |
299.348
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| Exact Mass |
299.073
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| CAS # |
26130-02-9
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| PubChem CID |
33334
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| Appearance |
White to off-white solid powder
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| Density |
1.42g/cm3
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| Index of Refraction |
1.752
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| LogP |
4.035
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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 |
3
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| Heavy Atom Count |
21
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| Complexity |
363
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JHBWYQRKOUBPCA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H13N3O2S/c1-20-11-7-8-12-13(9-11)21-15(17-12)18-14(19)16-10-5-3-2-4-6-10/h2-9H,1H3,(H2,16,17,18,19)
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| Chemical Name |
1-(6-methoxy-1,3-benzothiazol-2-yl)-3-phenylurea
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| Synonyms |
LY-53616; LY53616; LY 53616
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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 : ~12.5 mg/mL (~41.76 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (4.18 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 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: 1.25 mg/mL (4.18 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 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 | 3.3406 mL | 16.7029 mL | 33.4057 mL | |
| 5 mM | 0.6681 mL | 3.3406 mL | 6.6811 mL | |
| 10 mM | 0.3341 mL | 1.6703 mL | 3.3406 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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