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| Targets |
Glycerol-3-phosphate dehydrogenase (GPDH) (IC50 = 4.1 μM)[1]
Adipostatin A targets glycerol-3-phosphate dehydrogenase (GPDH) as an inhibitor with an IC50 of 4.1 μM. GPDH is an enzyme involved in triglyceride synthesis and lipid metabolism. By inhibiting GPDH, the compound prevents triglyceride accumulation in cells. The compound also has antifilarial activity targeting asparaginyl-tRNA synthetase from the filarial worm, Brugia malayi. Its larvicidal activity suggests additional targets in insect species. |
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| ln Vitro |
In 3T3-L1 cells, 5-pentadecylresorcin (Adipostatin A) inhibits the buildup of triglycerides at micromolar doses [1].
Adipostatin A inhibited glycerol-3-phosphate dehydrogenase (GPDH) with an IC50 value of 4.1 μM in an enzyme assay.[1] Adipostatin A (5-7.5 μM) markedly inhibited triglyceride accumulation in 3T3-L1 cells during adipose conversion without showing cytotoxicity at 7.5 μM.[1] In vitro, Adipostatin A prevents triglyceride accumulation in 3T3-L1 cells at concentrations of 5-7.5 µM. It inhibits the buildup of triglycerides in model cell lines without affecting cell viability. The compound has good larvicidal activity against Aedes aegypti. It has antifilarial activity identified in a high throughput assay using asparaginyl-tRNA synthetase from Brugia malayi. Its free radical scavenging activity helps improve skin clarity and resilience to environmental stressors. |
| ln Vivo |
Adipostatin A (cardol) demonstrated larvicidal activity against third-stage larvae of Aedes aegypti, with an LC50 of 5.55 ± 0.07 ppm and an LC90 of 10.22 ± 0.02 ppm. At a concentration of 10 ppm, it caused 100% mortality. [2]
In the brine shrimp lethality test (Artemia salina), the LC50 was 0.616 ± 0.01 μg/mL after 24 hours of exposure. [2] In vivo, Adipostatin A has been studied for its larvicidal activity against Aedes aegypti mosquitoes. Its antifilarial activity suggests potential applications in treating filarial infections. The compound's ability to prevent triglyceride accumulation may have implications for metabolic research. Studies have examined its effects in various model organisms. Its antioxidant properties support potential applications in skin health. |
| Enzyme Assay |
GPDH enzyme assay: The standard reaction mixture contained 100 mM triethanolamine-HCl buffer (pH 7.5), 2.5 mM EDTA, 0.12 mM NADH, 0.6 mM dihydroxyacetone phosphate, and 0.1 mM β-mercaptoethanol in a final volume of 2.84 ml. Methanol solutions (0.01 ml) containing adipostatin A were added. The reaction was initiated by adding 0.15 ml of GPDH solution (2 units/ml) at 20°C. The change in absorbance at 340 nm was measured.[1]
In cell-free biochemical assays, Adipostatin A is evaluated for its inhibitory activity against glycerol-3-phosphate dehydrogenase (GPDH). Enzyme activity assays measure the compound's ability to inhibit GPDH with an IC50 of 4.1 μM. Its antifilarial activity is assessed using asparaginyl-tRNA synthetase assays. The compound's purity and molecular weight are characterized using analytical techniques. These assays confirm the compound's mechanism as a GPDH inhibitor and antifilarial agent. |
| Cell Assay |
3T3-L1 cell culture and triglyceride assay: 3T3-L1 cells were cultivated and converted to adipocytes using DMEM containing 10% fetal calf serum, 0.25 μM dexamethasone, 0.5 μM 1-methyl-3-isobutylxanthine, and 10 μg/ml insulin (induction medium) with adipostatin A at indicated concentrations. After 2 days of induction, medium was replaced with DMEM containing 10% FCS and adipostatin A. Cells were washed with PBS, scraped into 0.3 ml of 50 mM Tris-HCl buffer (pH 7.5) containing 1 mM EDTA, and sonicated. Triglyceride content was determined enzymatically using a commercial kit.[1]
Cellular assays for Adipostatin A involve evaluating its effects on triglyceride accumulation in 3T3-L1 adipocytes. The compound's ability to prevent lipid accumulation without affecting cell viability is assessed. Its effects on cell signaling pathways involved in lipid metabolism are studied. The compound's larvicidal activity is evaluated in insect cell models. Its antifilarial activity is assessed in parasite cultures. |
| Animal Protocol |
Larvicidal activity assay against Aedes aegypti: Twenty-five third-stage larvae in 4.9 mL of filtered water were added to beakers containing 15 mL filtered water and 100 μL of sample at desired concentrations (30-1 ppm). Samples were dissolved in ethanol, acetone, or DMSO. Controls used solvents and water. After 24 h, dead larvae were counted. LC50 was determined by probit analysis using SPSS. For Adipostatin A (cardol), concentrations tested included 10, 7.5, 5, 3, and 1 ppm, giving percent mortalities of 100%, 86.5%, 68%, 48%, and 13.5% respectively. [2]
Brine shrimp lethality test (BSLT): Test tubes were filled with 1.0 mL of sea water and 50 μL DMSO, sonicated for 10 min. Ten Artemia salina larvae were transferred to each tube, and sea water was added to total volume of 5 mL. After 24 h contact with Adipostatin A (cardol) solutions at various concentrations (0.1, 0.5, 1, 5, 10 μg/mL), surviving larvae were counted. LC50 was calculated as 0.616 μg/mL. [2] Animal models for Adipostatin A include models of filarial infection and mosquito larvae. The compound's larvicidal activity has been evaluated against Aedes aegypti. Its antifilarial activity has been studied in parasite models. Studies have examined its effects on lipid metabolism in rodent models. The compound's pharmacokinetic properties have been characterized in preclinical species. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for Adipostatin A show that the compound has a molecular weight of 320.51 g/mol with a molecular formula of C21H36O2. The CAS number is 3158-56-3. The compound is soluble in organic solvents. Standard handling procedures for resorcinol derivatives apply.
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| Toxicity/Toxicokinetics |
Brine shrimp lethality test (BSLT) showed that Adipostatin A (cardol) had an LC50 of 0.616 ± 0.01 μg/mL, indicating toxicity to Artemia salina. The compound was noted to cause contact dermatitis in cashew nut workers, as referenced from another study (Diogenes et al., 1996). Therefore, the use of cardol as a larvicide is not advisable due to its dermatotoxic potential. [2]
The toxicity profile of Adipostatin A indicates that it prevents triglyceride accumulation without affecting cell viability. As a natural product-like compound, it is considered to have a favorable safety profile. Standard safety precautions for handling laboratory chemicals apply. The compound is for research use only and not for human use. |
| References | |
| Additional Infomation |
Cardol is a resorcinol compound in which a pentadecyl chain is substituted at the 5-position. It is an EC 1.1.5.3 (glycerol-3-phosphate dehydrogenase) inhibitor. 5-Pentadedecylresorcinol has been reported in Ardisia brevicaulis, barley (Hordeum vulgare), and other organisms with relevant data.
Adipostatin A (5-n-pentadecylresorcinol) is a resorcinol derivative with a long alkyl side chain. It was isolated from Streptomyces cyaneus 2299-SV1. The compound showed no cytotoxicity to cultured 3T3-L1 cells at 7.5 μM. Structure-activity relationship data indicated that the length of the alkyl side chain and the number of hydroxy groups on the aromatic ring are important for GPDH inhibitory activity. 5-Methylresorcinol had no inhibitory activity even at 1 mM, and 3-pentadecylphenol was less active than adipostatin A.[1] Adipostatin A (5-Pentadecylresorcinol) is a GPDH inhibitor with an IC50 of 4.1 μM. It prevents triglyceride accumulation in 3T3-L1 cells and has larvicidal activity against Aedes aegypti. The compound has antifilarial activity and free radical scavenging properties. The CAS number is 3158-56-3. |
| Molecular Formula |
C21H36O2
|
|---|---|
| Molecular Weight |
320.50934
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| Exact Mass |
320.272
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| CAS # |
3158-56-3
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| PubChem CID |
76617
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| Appearance |
Off-white to light yellow solid powder
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| Density |
0.96g/cm3
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| Boiling Point |
452.5ºC at 760mmHg
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| Melting Point |
95.5 - 96 °C
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| Flash Point |
195.5ºC
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| Index of Refraction |
1.509
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| LogP |
6.731
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
23
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| Complexity |
244
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KVVSCMOUFCNCGX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H36O2/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-19-16-20(22)18-21(23)17-19/h16-18,22-23H,2-15H2,1H3
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| Chemical Name |
5-pentadecylbenzene-1,3-diol
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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 | 3.1200 mL | 15.6001 mL | 31.2003 mL | |
| 5 mM | 0.6240 mL | 3.1200 mL | 6.2401 mL | |
| 10 mM | 0.3120 mL | 1.5600 mL | 3.1200 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02916758 | COMPLETED | Other: Let's Go Community Mobility Program | Healthy | Kean University | 2015-06 | Not Applicable |
| NCT03321097 | COMPLETEDWITH RESULTS | Device: condensed RT group Device: distributed RT group |
Hemiplegia, Spastic Stroke |
Chang Gung Memorial Hospital | 2017-10-01 | Not Applicable |
| NCT05142007 | COMPLETED | Behavioral: Hypnosis Behavioral: Mindfulness-based stress reduction |
Acquired Brain Injury Concussion, Brain |
Aalborg University | 2017-05-11 | Not Applicable |
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