| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
IC50: Lactate dehydrogenase
The primary target of Glomeratose A is lactate dehydrogenase (LDH), an enzyme involved in the conversion of pyruvate to lactate during glycolysis. By inhibiting LDH, the compound reduces lactate production and influences cellular metabolism. This property makes it significant for research into metabolic diseases and cancer treatment, as cancer cells often rely on aerobic glycolysis (the Warburg effect). |
|---|---|
| ln Vitro |
In vitro, Glomeratose A acts as a potent inhibitor of lactate dehydrogenase, reducing lactate production in cells. Its inhibitory effects on LDH have been characterized, and the compound demonstrates potential for modulating metabolic processes in cancer cells that exhibit elevated lactate levels. The compound also modulates NF-κB and MAPK signaling pathways.
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| ln Vivo |
In vivo studies on Glomeratose A are limited. Based on its mechanism of action as an LDH inhibitor, the compound may have therapeutic potential in conditions characterized by elevated lactate levels, such as certain cancers and metabolic disorders. Further in vivo studies are needed to fully characterize its pharmacological effects and therapeutic potential.
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| Enzyme Assay |
For in vitro enzyme inhibition assays, Glomeratose A is tested against recombinant lactate dehydrogenase. The enzyme is incubated with varying concentrations of the compound and its substrate (pyruvate) in the presence of NADH. LDH activity is measured by monitoring the decrease in absorbance at 340 nm due to NADH oxidation. IC₅₀ values are calculated from dose-response curves to determine the inhibitory potency.
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| Cell Assay |
For in vitro cell-based assays, Glomeratose A is typically tested on cancer cell lines that exhibit high glycolytic activity. Cells are treated with the compound at various concentrations (typically 1-100 μM) for 24-72 hours. Lactate production in the culture medium is measured using a lactate assay kit. Cell viability and proliferation are assessed using MTT or CCK-8 assays to evaluate the anti-proliferative effects.
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| Animal Protocol |
In vivo animal experiments for Glomeratose A have not been extensively reported. Based on its mechanism as an LDH inhibitor, potential experimental models include xenograft tumor models in mice to evaluate anti-tumor efficacy. The compound could be administered orally or intraperitoneally, with tumor volume measurements and lactate levels in tumor tissues assessed as pharmacodynamic endpoints.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Glomeratose A are not available in the published literature. As a glycoside natural product with a molecular weight of 562.52 g/mol and molecular formula C₂₄H₃₄O₁₅, it is expected to have moderate oral bioavailability. Standard pharmacokinetic studies would be required to determine its absorption, distribution, metabolism, and excretion profile.
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| Toxicity/Toxicokinetics |
Toxicological data for Glomeratose A are limited. As a natural product isolate, it is generally considered to have low toxicity at pharmacological doses. However, comprehensive toxicological studies have not been reported. The compound is classified as a research-grade reagent and is not for human use. Standard laboratory safety practices should be followed when handling.
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| References | |
| Additional Infomation |
Glomeratose A is a hydroxycinnamic acid. It has been reported to exist in Polygala glomerata, Polygala karensium, and Polygala sibirica, and relevant data are available.
Glomeratose A is a research-use only compound and has not been approved for clinical applications. It is also known as球腺糖A in Chinese. The compound is isolated from Polygala tenuifolia and belongs to the class of hydroxycinnamic acids. It is available from various research chemical suppliers. Its molecular weight is 562.52 and formula is C₂₄H₃₄O₁₅. |
| Molecular Formula |
C24H34O15
|
|---|---|
| Molecular Weight |
562.5178
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| Exact Mass |
562.189
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| CAS # |
202471-84-9
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| PubChem CID |
11972358
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| Appearance |
White to off-white solid
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
826.5±65.0 °C at 760 mmHg
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| Flash Point |
274.9±27.8 °C
|
| Vapour Pressure |
0.0±3.2 mmHg at 25°C
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| Index of Refraction |
1.626
|
| Source |
Originated from plants: Polygalaceae Polygala tenuifolia Willd.
|
| LogP |
-1.33
|
| Hydrogen Bond Donor Count |
7
|
| Hydrogen Bond Acceptor Count |
15
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
39
|
| Complexity |
798
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| Defined Atom Stereocenter Count |
9
|
| SMILES |
O1[C@H](CO)[C@H]([C@@H]([C@@]1(CO)O[C@@H]1[C@@H]([C@H]([C@@H]([C@@H](CO)O1)O)O)O)OC(/C=C/C1C=C(C(=C(C=1)OC)OC)OC)=O)O
|
| InChi Key |
PQHNJDATPYXLIX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H34O15/c1-33-12-6-11(7-13(34-2)21(12)35-3)4-5-16(28)37-22-18(30)15(9-26)38-24(22,10-27)39-23-20(32)19(31)17(29)14(8-25)36-23/h4-7,14-15,17-20,22-23,25-27,29-32H,8-10H2,1-3H3
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| Chemical Name |
[4-hydroxy-2,5-bis(hydroxymethyl)-2-[3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxolan-3-yl] 3-(3,4,5-trimethoxyphenyl)prop-2-enoate
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~177.77 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.44 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 (4.44 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7777 mL | 8.8886 mL | 17.7771 mL | |
| 5 mM | 0.3555 mL | 1.7777 mL | 3.5554 mL | |
| 10 mM | 0.1778 mL | 0.8889 mL | 1.7777 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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