| Size | Price | Stock | Qty |
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| 5mg |
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| 100mg |
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| Targets |
Ruscogenin targets multiple inflammatory pathways. It suppresses TXNIP/NLRP3 inflammasome activation and the MAPK pathway, reducing inflammation and oxidative stress. Ruscogenin inhibits the expression of tissue factor (TF), inducible nitric oxide synthase (iNOS), and NF-κB p65, which are key mediators of inflammation and thrombosis. It also inhibits leukocyte adhesion to endothelial cells in a concentration-dependent manner. These actions contribute to its anti-inflammatory and anti-thrombotic effects.
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| ln Vitro |
Ruscogenin (0.01–40 μM; 24 hours) can improve bEnd.3 cell viability when treated with OGD/R [1]. Ruscogenin (0.01–10 μM; 24 hours) can improve bEnd.3 cell viability when treated with OGD/R [1]. It has the ability to decrease the TXNIP/NLRP3 dye signal, block the expression of IL-Iβ and Caspase-1, and restore endothelial cell barrier leakage [1]. OGD/R-treated bEnd.3 treated with ruscovenin (0.01-10 μM; 4 hours)
In vitro, ruscogenin inhibits the expression of TF, iNOS, and NF-κB p65. It remarkably inhibits adhesion of leukocytes to human umbilical vein endothelial cells (ECV304) injured by TNF-α in a concentration-dependent manner. Ruscogenin's anti-inflammatory activity has been demonstrated in cell-based assays measuring inflammatory cytokine production and adhesion molecule expression. Its ability to suppress TXNIP/NLRP3 inflammasome activation has been confirmed in various cell models. |
| ln Vivo |
Ruscogenin (10 mg/kg; gavage; once) reduces MCAO/R-induced brain tissue damage, stops IL-1β and Caspase-1 production, and prevents TXNIP/NLRP3 activation [1].
In vivo, ruscogenin has anti-inflammatory activity and suppresses zymosan A-evoked peritoneal total leukocyte migration in mice in a dose-dependent manner. It attenuates cerebral ischemia-induced blood-brain barrier dysfunction. Ruscogenin also exerts significant anti-thrombotic activities. It has been studied for its potential in treating acute lung injury and sepsis. However, specific experimental details are limited in the available literature. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for ruscogenin are not typical because it modulates multiple pathways rather than a single enzyme. However, its ability to inhibit iNOS activity can be assessed using enzyme activity assays with purified iNOS. NF-κB activation can be assessed using electrophoretic mobility shift assays (EMSA) or luciferase reporter assays. TXNIP/NLRP3 inflammasome activation can be assessed by measuring caspase-1 activity and IL-1β production.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: bEnd.3 cell Tested Concentrations: 0.01 μM, 0.1 μM, 1 μM, 10 μM, 20 μM, 40 μM Incubation Duration: 24 hrs (hours) Experimental Results: It shows that the decrease in cell viability induced by OGD/R in bEnd.3 cells is Dramatically restored. Immunofluorescence [1] Cell Types: bEnd.3 Cell Tested Concentrations: 0.1 μM, 1 μM, 10 μM Incubation Duration: 24 h Experimental Results: Shows increased TEER value and inhibits fluorescein sodium permeability. Western Blot Analysis[1] Cell Types: bEnd.3 Cell Tested Concentrations: 0.01 μM, 0.1 μM, 1 μM, 10 μM, 20 μM, 40 μM Incubation Duration: 24 h Experimental Results: IL-1β and Caspase expression down-regulated -1 protein, and inhibited the expression of NLRP3 and TXNIP. Immunofluorescence[1] Cell Types: bEnd.3 Cell Tested Concentrations: 0.01 μM, 0.1 μM, 1 μM, 10 μM, 20 μM, 40 μM Incubation Duration: 4 hrs (hours) Experimental Results: Demonstrated diminished ROS production. In vitro cellular assays for ruscogenin are performed using endothelial cells (e.g., ECV304) or macrophages. Cells are treated with ruscogenin and stimulated with TNF-α or LPS. Leukocyte adhesion is assessed by counting adherent cells. Inflammatory cytokine production (IL-1β, TNF-α) is measured by ELISA. NF-κB activation is assessed by Western blotting for p65 nuclear translocation. iNOS expression is measured by Western blotting or quantitative PCR. |
| Animal Protocol |
Animal/Disease Models: MCAO/R mice [1]
Doses: 10mg/kg Route of Administration: po (oral gavage) (ig) Experimental Results: Smaller infarct size, improved histopathological damage by reducing cell loss, CBF (brain blood flow) Dramatically increased in the model group. Results Compared with the model group, the expressions of IL-1β, Caspase-1, NLRP3 and TXNIP were inhibited. In vivo animal experiments for ruscogenin are conducted in mouse models of peritonitis and cerebral ischemia. Mice are administered ruscogenin via oral or intraperitoneal injection, and zymosan A is injected into the peritoneal cavity to induce inflammation. Peritoneal leukocyte migration is assessed by counting cells in the peritoneal lavage fluid. In cerebral ischemia models, blood-brain barrier integrity is assessed by measuring Evans blue extravasation. |
| ADME/Pharmacokinetics |
Ruscogenin has a molecular weight of 430.62 g/mol and a molecular formula of C27H42O4. It is an important steroid sapogenin derived from Ophiopogon japonicus. The compound should be stored under recommended conditions. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability have not been extensively reported. As a natural product, ruscogenin may have limited oral bioavailability.
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| Toxicity/Toxicokinetics |
The toxicological profile of ruscogenin has not been extensively characterized. As a steroidal sapogenin, the compound may have potential endocrine effects at high doses. No significant toxicity has been reported in the available literature. Comprehensive toxicology studies would be necessary to fully assess its safety for clinical development. The compound is generally considered safe for research use.
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| References |
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| Additional Infomation |
Ruscogenin is a triterpenoid compound. It has been reported to be found in Tribulus terrestris, Cordyline banksii, and other organisms with relevant data.
Ruscogenin is an important steroidal sapogenin with significant anti-inflammatory and anti-thrombotic activities. It is derived from Ophiopogon japonicus (maidong) and Ruscus aculeatus. Ruscogenin attenuates cerebral ischemia-induced blood-brain barrier dysfunction by suppressing TXNIP/NLRP3 inflammasome activation and the MAPK pathway. It also inhibits the expression of TF, iNOS, and NF-κB p65. Ruscogenin is a research compound with potential applications in inflammation and thrombosis. |
| Molecular Formula |
C27H42O4
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| Molecular Weight |
430.6200
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| Exact Mass |
430.308
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| CAS # |
472-11-7
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| PubChem CID |
441893
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
563.1±50.0 °C at 760 mmHg
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| Melting Point |
198-202ºC
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| Flash Point |
294.4±30.1 °C
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| Vapour Pressure |
0.0±3.5 mmHg at 25°C
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| Index of Refraction |
1.577
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| LogP |
4.29
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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 |
0
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| Heavy Atom Count |
31
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| Complexity |
779
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| Defined Atom Stereocenter Count |
12
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| SMILES |
C[C@@H]1CC[C@@]2([C@H]([C@H]3[C@@H](O2)C[C@@H]4[C@@]3(CC[C@H]5[C@H]4CC=C6[C@@]5([C@@H](C[C@@H](C6)O)O)C)C)C)OC1
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| InChi Key |
QMQIQBOGXYYATH-IDABPMKMSA-N
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| InChi Code |
InChI=1S/C27H42O4/c1-15-7-10-27(30-14-15)16(2)24-22(31-27)13-21-19-6-5-17-11-18(28)12-23(29)26(17,4)20(19)8-9-25(21,24)3/h5,15-16,18-24,28-29H,6-14H2,1-4H3/t15-,16+,18-,19-,20+,21+,22+,23-,24+,25+,26+,27-/m1/s1
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| Chemical Name |
(1S,2S,4S,5'R,6R,7S,8R,9S,12S,13R,14R,16R)-5',7,9,13-tetramethylspiro[5-oxapentacyclo[10.8.0.02,9.04,8.013,18]icos-18-ene-6,2'-oxane]-14,16-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 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 : ~25 mg/mL (~58.06 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.83 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 (4.83 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.83 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 | 2.3222 mL | 11.6112 mL | 23.2223 mL | |
| 5 mM | 0.4644 mL | 2.3222 mL | 4.6445 mL | |
| 10 mM | 0.2322 mL | 1.1611 mL | 2.3222 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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