| Size | Price | Stock | Qty |
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| Targets |
L-type calcium channel
Urolithin C targets multiple molecular pathways involved in metabolism and cell death. It acts as a glucose-dependent activator of insulin secretion by facilitating L-type Ca2+ channel opening and Ca2+ influx into pancreatic β-cells. Urolithin C enhanced glucose-induced extracellular signal-regulated kinases 1/2 (ERK1/2) activation as shown by higher phosphorylation levels in INS-1 β-cells. The compound is also an allosteric inhibitor of liver-specific pyruvate kinase (PKL), affecting glucose metabolism. Urolithin C induces apoptosis through a mitochondria-mediated pathway and stimulates ROS formation. In a cellular antioxidant assay, urolithin C demonstrates the most potent activity among tested urolithins and parent compounds. |
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| ln Vitro |
In INS-1 beta cells, urolithin C (20–100 μM; 1 hour) administration increases glucose-induced extracellular signal-regulated kinase 1/2 (ERK1/2) activation [1]. Significant inhibition of PC12 cell growth was seen with urolithin C. Treatment with urolithin C produces abnormalities related to calcium homeostasis, accelerates the generation of reactive oxygen species (ROS) and mitochondrial membrane depolarization, and increases the release of lactate dehydrogenase (LDH) and lipid peroxidation malondialdehyde (MDA) [2]. Treatment with urolithin C causes S-phase cell cycle arrest and apoptosis [2]
In vitro, urolithin C has demonstrated multiple biological activities. It acts as a glucose-dependent activator of insulin secretion and enhances glucose-induced ERK1/2 activation in INS-1 β-cells. Urolithin C is an L-type Ca2+ channel opener that enhances Ca2+ influx. It is also an allosteric inhibitor of liver-specific pyruvate kinase (PKL). The compound induces apoptosis through a mitochondria-mediated pathway and stimulates ROS formation. In a cellular antioxidant assay, urolithin C demonstrates the most potent activity among tested urolithins. The compound inhibits cell proliferation. These diverse activities make urolithin C a compound of interest for metabolic and cancer research. |
| ln Vivo |
Male Wistar rats weighing 140–160 g were used to study the pharmacokinetics of urolithin C (10 mg/kg; intraperitoneally given). The terminal fraction has a half-life of 11.3 hours and a total clearance (CL/F) of 3.41 L/h/kg. The distribution's initial volume (V1/F) and steady-state volume (Vss/F) are, respectively, 0.831 L/kg and 55.6 L/kg[3].
In vivo, urolithin C has been studied for its effects on metabolism and cell death. As a gut-microbial metabolite of ellagic acid, it is produced in the gastrointestinal tract and can be absorbed into the circulation. Its glucose-dependent activation of insulin secretion suggests potential for improving glucose metabolism. The compound's ability to induce apoptosis through a mitochondria-mediated pathway indicates potential anticancer activity. Urolithin C's effects on ROS formation may contribute to both its beneficial and toxic effects. Detailed in vivo studies are described in the primary literature. The compound's activity as a potent antioxidant suggests potential for protecting against oxidative stress-related diseases. |
| Enzyme Assay |
For in vitro biochemical assays, urolithin C is evaluated for its effects on various targets. Ca2+ channel opening activity is assessed using fluorescence-based calcium influx assays or patch-clamp electrophysiology. Insulin secretion is measured using ELISA or radioimmunoassay in INS-1 β-cells. ERK1/2 phosphorylation is assessed by Western blotting. Pyruvate kinase inhibition is measured using enzyme activity assays. Apoptosis is assessed by measuring caspase activity, DNA fragmentation, and mitochondrial membrane potential. ROS production is measured using fluorescent probes such as DCFH-DA. Antioxidant activity is evaluated using DPPH, ABTS, or cellular antioxidant assays. These cell-free and cell-based assays help characterize the compound's multiple biological activities.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: INS-1 cells Tested Concentrations: 20 μM, 100 μM Incubation Duration: 1 hour Experimental Results: Enhanced glucose-induced extracellular signal-regulated kinases 1/2 (ERK1/2) activation. In vitro cellular assays for urolithin C are performed using various cell lines including INS-1 pancreatic β-cells, PC12 cells, and other cell types. Cells are cultured in standard media and treated with urolithin C at various concentrations. Insulin secretion is measured using ELISA. Ca2+ influx is assessed using fluorescent calcium indicators. ERK1/2 phosphorylation is analyzed by Western blotting. Apoptosis is evaluated by measuring caspase activity, Annexin V/PI staining, and mitochondrial membrane potential using JC-1 staining. ROS production is detected using DCFH-DA fluorescent probes. Cell viability and proliferation are assessed using MTT or CCK-8 assays. These cellular assays help validate the compound's metabolic and pro-apoptotic activities. |
| Animal Protocol |
In vivo animal experiments with urolithin C are conducted to study its metabolic and anticancer effects. Rodent models of diabetes or metabolic syndrome can be used to assess effects on glucose metabolism and insulin secretion. Tumor xenograft models can be employed to evaluate anticancer activity. Urolithin C is administered via oral gavage, intraperitoneal injection, or intravenous injection at doses determined from pharmacokinetic studies. Efficacy endpoints include blood glucose levels, insulin levels, glucose tolerance, tumor growth inhibition, and survival. Tissue samples are analyzed for markers of apoptosis, ROS, and metabolic pathways. The compound's antioxidant activity can be assessed by measuring oxidative stress markers in tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of urolithin C have been characterized in studies of ellagic acid metabolism. As a gut-microbial metabolite, urolithin C is produced in the gastrointestinal tract and absorbed into the circulation. Its bioavailability depends on the gut microbiome composition and the presence of ellagic acid precursors. Urolithin C has a molecular weight of 244.20 and is expected to have moderate oral bioavailability. The compound is distributed to various tissues including liver, adipose tissue, and brain. It is metabolized and eliminated through conjugation and renal excretion. Detailed PK parameters such as half-life, Cmax, Tmax, AUC, volume of distribution, and clearance are available in the primary literature.
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| Toxicity/Toxicokinetics |
The toxicological profile of urolithin C is not extensively characterized. As a gut-microbial metabolite of ellagic acid, it is a naturally occurring compound that is generally considered safe. However, its ability to induce apoptosis through a mitochondria-mediated pathway and stimulate ROS formation suggests potential for cytotoxicity at high concentrations. The compound's pro-apoptotic activity may be beneficial in cancer cells but could be toxic to normal cells at high doses. Comprehensive toxicity studies including acute, subchronic, and chronic toxicity assessments are limited. The compound is intended for research use only and not for human therapeutic applications without appropriate safety evaluation. Researchers should follow standard laboratory safety practices when handling urolithin C.
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| References |
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| Additional Infomation |
Urolithin C is a coumarin compound. It has been reported that urolithin C has been found in pomegranate (Punica granatum), and relevant data are available for reference.
Urolithin C is a valuable research tool for studying glucose metabolism, insulin secretion, and apoptosis. Its glucose-dependent activation of insulin secretion makes it useful for investigating the mechanisms of insulin release and developing therapies for diabetes. The compound's L-type Ca2+ channel opening activity provides opportunities for studying calcium signaling in pancreatic β-cells. Its inhibition of pyruvate kinase makes it relevant for studying glucose metabolism and cancer metabolism. Urolithin C's pro-apoptotic activity can be employed to study mitochondria-mediated apoptosis and develop anticancer strategies. Its potent antioxidant activity makes it useful for studying oxidative stress and developing antioxidant therapies. The compound's origin as a gut-microbial metabolite makes it relevant for studying the gut microbiome and its effects on host metabolism. |
| Molecular Formula |
C13H8O5
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|---|---|
| Molecular Weight |
244.20
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| Exact Mass |
244.037
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| CAS # |
165393-06-6
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| PubChem CID |
60198001
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| Appearance |
Light brown to brown solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
605.4±55.0 °C at 760 mmHg
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| Flash Point |
243.6±25.0 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.758
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| LogP |
1.88
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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 |
0
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| Heavy Atom Count |
18
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| Complexity |
344
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HHXMEXZVPJFAIJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H8O5/c14-6-1-2-7-8-4-10(15)11(16)5-9(8)13(17)18-12(7)3-6/h1-5,14-16H
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| Chemical Name |
3,8,9-trihydroxybenzo[c]chromen-6-one
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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 : 50 mg/mL (204.75 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.52 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 20.8 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: ≥ 2.08 mg/mL (8.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0950 mL | 20.4750 mL | 40.9500 mL | |
| 5 mM | 0.8190 mL | 4.0950 mL | 8.1900 mL | |
| 10 mM | 0.4095 mL | 2.0475 mL | 4.0950 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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