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| Targets |
Notoginsenoside R2 targets the MEK1/2-ERK1/2 signaling pathway. By activating this pathway, it leads to the activation of downstream targets such as P90RSK and Nrf2. Nrf2 is a master regulator of the antioxidant response, and its activation leads to the expression of cytoprotective genes. This mechanism underlies its neuroprotective, antioxidant, and anti-inflammatory effects. It also modulates the PI3K/Akt and MAPK pathways.
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| ln Vitro |
In vitro, Notoginsenoside R2 has protective effects on 6-OHDA-induced oxidative stress and apoptosis. Its neuroprotection is associated with P90RSK and Nrf2 activation through MEK1/2-ERK1/2 pathways. It also exerts anti-inflammatory, antioxidant, and cytoprotective effects. These in vitro studies demonstrate its potential as a neuroprotective and cytoprotective agent.
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| ln Vivo |
In vivo activity data for Notoginsenoside R2 is limited in publicly available literature. As a compound with potent neuroprotective and antioxidant effects in vitro, it is hypothesized to exhibit similar effects in animal models of neurodegenerative diseases. However, specific in vivo efficacy studies, including pharmacokinetic and pharmacodynamic parameters, have not been detailed in the available sources. Further research is needed to fully characterize its in vivo activity.
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| Enzyme Assay |
For cell-free enzyme assays, the activity of Notoginsenoside R2 can be studied using kinase activity assays for its targets, such as MEK1/2 or ERK1/2. The compound is incubated with the purified kinase and its substrate in the presence of ATP. The phosphorylation of the substrate is measured using radioactive or fluorescence-based methods.
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| Cell Assay |
For in vitro cellular assays, the neuroprotective effect of Notoginsenoside R2 is assessed in neuronal cell models exposed to 6-OHDA-induced toxicity. Cells are treated with the compound prior to or concurrently with 6-OHDA. Cell viability is measured using MTT or other assays. The activation of the MEK1/2-ERK1/2 pathway and the expression of Nrf2 and its target genes are measured by Western blot or qPCR.
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| Animal Protocol |
For in vivo studies, Notoginsenoside R2 could be administered orally or intraperitoneally in rodent models of Parkinson's disease or other neurodegenerative disorders. Its neuroprotective effect would be assessed by measuring behavioral outcomes, neuronal survival, and markers of oxidative stress and inflammation in the brain.
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| ADME/Pharmacokinetics |
Notoginsenoside R2 has a molecular formula of C41H70O13 and a molecular weight of 771 g/mol. Its CAS number is 80418-25-3. It is a triterpenoid saponin and is typically supplied as a powder. It is soluble in DMSO and ethanol. For in vitro studies, stock solutions are prepared in DMSO. For in vivo administration, it can be formulated in suitable vehicles. Storage is recommended at 2-8°C for up to 24 months. Its purity is typically >98% for research use.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As a natural saponin, its safety profile would need to be established through standard toxicological studies. In vitro cytotoxicity assays in various cell lines are typically performed alongside efficacy studies to confirm that the observed effects are not due to a general reduction in cell viability.
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| References |
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| Additional Infomation |
Panax notoginseng saponin R2 is a triterpenoid saponin. It has been reported that Panax notoginseng saponin R2 exists in Japanese ginseng and Panax notoginseng, and relevant data are available for reference.
Notoginsenoside R2 is a research-grade compound and is not approved for any therapeutic use. It serves primarily as a valuable pharmacological tool for studying neuroprotection and the mechanisms of ginsenosides. Its mechanism of action involves the activation of the MEK1/2-ERK1/2 pathway and the upregulation of Nrf2-mediated antioxidant responses. Its neuroprotective and antioxidant activities make it a compound of interest for drug discovery. No clinical trials have been reported. |
| Molecular Formula |
C41H70O13
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|---|---|
| Molecular Weight |
770.9867
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| Exact Mass |
770.481
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| CAS # |
80418-25-3
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| PubChem CID |
21599925
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
878.7±65.0 °C at 760 mmHg
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| Flash Point |
485.2±34.3 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.597
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| LogP |
6.45
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
54
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| Complexity |
1360
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| Defined Atom Stereocenter Count |
20
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| SMILES |
CC(=CCC[C@@](C)([C@H]1CC[C@@]2([C@@H]1[C@@H](C[C@H]3[C@]2(C[C@@H]([C@@H]4[C@@]3(CC[C@@H](C4(C)C)O)C)O[C@H]5[C@@H]([C@H]([C@@H]([C@H](O5)CO)O)O)O[C@H]6[C@@H]([C@H]([C@@H](CO6)O)O)O)C)O)C)O)C
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| InChi Key |
FNIRVWPHRMMRQI-PGOMJGFXSA-N
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| InChi Code |
InChI=1S/C41H70O13/c1-20(2)10-9-13-41(8,50)21-11-15-39(6)28(21)22(43)16-26-38(5)14-12-27(45)37(3,4)34(38)24(17-40(26,39)7)52-36-33(31(48)30(47)25(18-42)53-36)54-35-32(49)29(46)23(44)19-51-35/h10,21-36,42-50H,9,11-19H2,1-8H3/t21-,22+,23+,24-,25+,26+,27-,28-,29-,30+,31-,32+,33+,34-,35-,36+,38+,39+,40+,41-/m0/s1
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| Chemical Name |
(2S,3R,4S,5R)-2-[(2R,3R,4S,5S,6R)-2-[[(3S,5R,6S,8R,9R,10R,12R,13R,14R,17S)-3,12-dihydroxy-17-[(2S)-2-hydroxy-6-methylhept-5-en-2-yl]-4,4,8,10,14-pentamethyl-2,3,5,6,7,9,11,12,13,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-6-yl]oxy]-4,5-dihydroxy-6-(hydroxymethyl)oxan-3-yl]oxyoxane-3,4,5-triol
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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 (~129.70 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.24 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 (3.24 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 (3.24 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 | 1.2970 mL | 6.4852 mL | 12.9703 mL | |
| 5 mM | 0.2594 mL | 1.2970 mL | 2.5941 mL | |
| 10 mM | 0.1297 mL | 0.6485 mL | 1.2970 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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