| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg | |||
| Other Sizes |
| Targets |
The primary target of Gypenoside XLIX is the peroxisome proliferator-activated receptor alpha (PPAR-α). It acts as a selective activator of this nuclear receptor. By activating PPAR-α, the compound regulates the expression of genes involved in lipid metabolism, inflammation, and energy homeostasis. It inhibits cytokine-induced vascular cell adhesion molecule-1 (VCAM-1) overexpression and hyperactivity in human endothelial cells. It also inhibits LPS-induced tissue factor (TF) overexpression in human THP-1 monocytic cells via PPAR-α-dependent pathways. Furthermore, Gypenoside XLIX effectively inhibits the TLR4-mediated NF-κB signaling pathway, reducing reactive oxygen species (ROS) accumulation.
|
|---|---|
| ln Vitro |
In vitro, Gypenoside XLIX has demonstrated significant anti-inflammatory and antioxidative activities. It inhibits cytokine-induced VCAM-1 expression and activity in human endothelial cells. It also inhibits LPS-induced TF overexpression in human THP-1 monocytic cells. The compound's ability to inhibit the TLR4-mediated NF-κB signaling pathway and reduce ROS accumulation contributes to its anti-inflammatory effects. These activities suggest that Gypenoside XLIX can protect endothelial cells and monocytes from inflammatory damage.
|
| ln Vivo |
In vivo, Gypenoside XLIX has shown promise in the treatment of metabolic disorders such as type 2 diabetes and NAFLD. In a rat model, it has been shown to ameliorate various conditions, including sepsis-induced liver, kidney, and splenic injuries. Its ability to activate PPAR-α and inhibit inflammatory pathways contributes to its therapeutic effects. However, detailed in vivo efficacy data are not extensively documented in the public literature. Further studies are needed to fully characterize its therapeutic potential.
|
| Enzyme Assay |
For in vitro enzyme assays, the activity of Gypenoside XLIX as a PPAR-α activator can be assessed using cell-based reporter gene assays. Cells are transfected with a PPAR-α expression plasmid and a luciferase reporter gene driven by a PPAR response element (PPRE). The compound's ability to activate the receptor is measured by the increase in luciferase activity. The compound's effects on VCAM-1 expression can be assessed by Western blotting or ELISA.
|
| Cell Assay |
For in vitro cell-based assays, the anti-inflammatory activity of Gypenoside XLIX is evaluated using human endothelial cells or THP-1 monocytic cells. Cells are stimulated with inflammatory cytokines (e.g., TNF-α) or LPS in the presence of the compound. The expression of VCAM-1, TF, and other inflammatory markers is measured by Western blotting, qPCR, or ELISA. The compound's effects on NF-κB signaling are assessed by measuring the phosphorylation of IκB and the nuclear translocation of NF-κB. ROS accumulation is measured using fluorescent probes.
|
| Animal Protocol |
For in vivo animal studies, Gypenoside XLIX is typically administered orally in rodent models of metabolic or inflammatory diseases. In models of type 2 diabetes or NAFLD, animals are treated with the compound, and parameters such as blood glucose, insulin sensitivity, lipid profiles, and liver histology are assessed. In models of sepsis, animals are treated with the compound, and organ injury and inflammatory markers are assessed.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Gypenoside XLIX: The compound is a dammarane-type glycoside and exhibits amphiphilic properties. It demonstrates notable solubility in polar solvents. As a glycoside, it is expected to have limited oral bioavailability. Detailed pharmacokinetic parameters are not publicly available.
|
| Toxicity/Toxicokinetics |
Gypenoside XLIX is generally considered to have a favorable safety profile based on the traditional use of Gynostemma pentaphyllum. However, comprehensive toxicological studies have not been published. The compound is used for research purposes only and is not intended for human use. Standard laboratory safety precautions should be observed.
|
| References | |
| Additional Infomation |
Reports have indicated that Gynostemma pentaphyllum contains gypenosin XLIX, and relevant data is available for reference.
Gypenoside XLIX is a research compound with no clinical trial or regulatory approval status. It is a natural dammarane-type glycoside from Gynostemma pentaphyllum and is a selective PPAR-α activator. It is commercially available from chemical suppliers for research purposes only. The compound is of interest in the study of metabolic disorders, inflammation, and cardiovascular diseases. |
| Molecular Formula |
C52H86O21
|
|---|---|
| Molecular Weight |
1047.2267
|
| Exact Mass |
1046.566
|
| CAS # |
94987-08-3
|
| PubChem CID |
16007240
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
1105.1±65.0 °C at 760 mmHg
|
| Flash Point |
306.9±27.8 °C
|
| Vapour Pressure |
0.0±0.6 mmHg at 25°C
|
| Index of Refraction |
1.615
|
| LogP |
5.46
|
| Hydrogen Bond Donor Count |
12
|
| Hydrogen Bond Acceptor Count |
21
|
| Rotatable Bond Count |
15
|
| Heavy Atom Count |
73
|
| Complexity |
1910
|
| Defined Atom Stereocenter Count |
27
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~119.36 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (5.97 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 62.5 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: ≥ 6.25 mg/mL (5.97 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 62.5 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: ≥ 6.25 mg/mL (5.97 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 | 0.9549 mL | 4.7745 mL | 9.5490 mL | |
| 5 mM | 0.1910 mL | 0.9549 mL | 1.9098 mL | |
| 10 mM | 0.0955 mL | 0.4775 mL | 0.9549 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
