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| 5mg |
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| 10mg |
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| Targets |
Ginsenoside Rb2 targets multiple pathways and receptors. It upregulates GPR120 gene expression and is an inducer of the SOD1 gene through transcription factor AP2 binding sites. It activates AMPK pathways in HepG2 cells to regulate glucose metabolism and has been shown to inhibit CYP2C19 with an IC50 of 62 μmol/L. It also modulates glucocorticoid receptor activity and exerts anti-inflammatory effects through GPR120 activation.
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| ln Vitro |
The anti-inflammatory effects of α-terminal acid (ALA) are enhanced by ginsenoside Rb2, and this enhancement is fully reliant on GPR120 activation. On lipopolysaccharide (LPS)-stimulated macrophage RAW264.7 cells, ginsenoside Rb2 exhibits anti-inflammatory properties through upregulating GPR120 expression, which in turn amplifies ω-3-induced GPR120 activation. Ginsenoside Rb2 decreases cholesterol and triacylglycerol levels in 3T3-L1 cells by lowering oxidative damage and enhances circulation in liver cells by activating AMPK. The anti-UV properties of ginsenoside Rb2 are seen in mouse bone marrow mesenchymal stem cells (BMMSCs). The results of the MTT assay demonstrated that ginsenoside Rb2 (up to 100 μM) had no discernible effect on RAW264.7 cells, whether ALA was present or not. Ginsenoside Rb2 (0.1-100 μM; 12 h) was dependent on GPR120 expression being upregulated. GPR120 mRNA expression increased by 2.8 times when RAW264.7 macrophages were incubated with Ginsenoside Rb2 (10 μM) for a brief duration of 12 hours, according to real-time PCR data. Furthermore, ginsenoside Rb2 induced a time-dependent rise in GPR120 expression that began as early as 6 hours. According to these findings, Rb2 increases GPR120 expression in RAW264.7 macrophages in a time- and dose-dependent way [1].
In vitro, Ginsenoside Rb2 inhibits α-glucosidase with an IC50 of 32.2 μM and α-amylase with an IC50 of 128 μM. It inhibits TNF-α with an IC50 of 27.9±1.7 μM. Rb2 inhibits invasiveness of endometrial cancer cell lines Ishikawa to the basement membrane. It demonstrates antiviral activity with reported IC50 values in the micromolar concentration range. Rb2 pre-treatment enhances the anti-inflammatory effect of α-linolenic acid (ALA) in a strictly GPR120-dependent manner. |
| ln Vivo |
Rotavirus (RV) infection can be avoided with the antiviral drug ginsenoside Rb2. This ginsenoside treatment proved most successful when administered at a dose of 75 mg/kg three days before to viral challenge, even when varying doses of ginsenoside Rb2 (25 to 250 mg/kg) were provided three, two, or one day prior to viral challenge. minimizes diarrhea caused by the rotavirus (RV). Furthermore, it was found that administering ginsenoside Rb2 (75 mg/kg) continuously for 3, 2, and 1 days prior to viral infection was more effective than administering it only once on day 3. RV infections are destroyed when ginsenoside Rb2 is continuously formulated because it lowers viral titers [2].
In vivo, Ginsenoside Rb2 inhibits tumor growth and metastasis by disrupting angiogenesis. It regulates blood glucose levels and enhances cognitive function. Rb2 has shown protective effects against oxidative stress and supports cardiovascular health. It exhibits antioxidant and anticancer activities in various animal models, and its anti-inflammatory effects have been demonstrated through GPR120-mediated pathways. |
| Enzyme Assay |
The in vitro activity of Ginsenoside Rb2 is assessed using cell-free enzyme inhibition assays. For α-glucosidase inhibition, the enzyme is incubated with p-nitrophenyl-α-D-glucopyranoside substrate and varying concentrations of Rb2, and the release of p-nitrophenol is measured spectrophotometrically at 405 nm. For CYP inhibition assays, human liver microsomes are incubated with specific CYP substrates and NADPH in the presence of Rb2, and metabolite formation is analyzed by LC-MS/MS. GPR120 binding can be assessed using radioligand displacement assays with membrane preparations from GPR120-expressing cells.
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| Cell Assay |
For cellular assays, HepG2 hepatoma cells are cultured in DMEM with 10% FBS and treated with various concentrations of Rb2 (typically 1-200 μM) for 24-48 hours. Glucose uptake is measured using 2-NBDG fluorescent glucose analog. AMPK phosphorylation is analyzed by Western blotting using phospho-specific antibodies. For anti-inflammatory studies, cells are pre-treated with Rb2 before stimulation with inflammatory stimuli, and cytokine production is measured by ELISA. Endometrial cancer cell lines Ishikawa are used to assess anti-invasive activity using Matrigel invasion assays.
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| Animal Protocol |
In vivo, Ginsenoside Rb2 is typically administered orally or intraperitoneally to rodents at doses ranging from 10-100 mg/kg. In tumor xenograft models, mice bearing tumors are treated with Rb2 daily for 2-4 weeks, and tumor volume is monitored. Angiogenesis is assessed by immunohistochemical staining of CD31 in tumor tissues. For metabolic studies, diabetic mice are treated with Rb2, and fasting blood glucose, insulin levels, and glucose tolerance are measured. Tissue samples are collected for histopathological and biochemical analysis.
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| ADME/Pharmacokinetics |
Rb2 has a molecular weight of 1079.30 g/mol and is soluble in water at 10 mM. It is a white powder with >98% purity. The compound should be stored at -20°C, with a shelf life of 2 years from QC date when stored properly. Boiling point is 1117.1±65.0 °C, melting point is 197-199°C, and density is 1.4±0.1 g/cm³. Pharmacokinetic parameters such as bioavailability and half-life are not well-documented in the literature.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Ginsenoside Rb2 is limited in the provided search results. As a natural ginseng component, it is generally considered to have low toxicity. In vitro studies at concentrations up to 200 μM did not show significant cytotoxicity in HepG2 cells. The compound's IC50 for CYP2C19 inhibition (62 μmol/L) suggests potential for drug-drug interactions at high concentrations. Comprehensive toxicological studies are required to establish its full safety profile.
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| References |
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| Additional Infomation |
Ginsenoside Rb2 is a ginsenoside found in ginseng. Its structure is dammarane-type, with hydroxyl groups substituted at the 3β, 12β, and 20 pro-S positions. Specifically, the hydroxyl groups at positions 3 and 20 are converted to the corresponding β-D-glucopyranosyl-(1→2)-β-D-glucopyranoside and α-L-arabinopyranosyl-(1→6)-β-D-glucopyranoside, respectively, and a double bond is introduced at positions 24-25. It possesses activities as a plant metabolite, antiviral agent, and hypoglycemic agent. It is a 12β-hydroxysteroid, β-D-glucoside, disaccharide derivative, ginsenoside, and tetracyclic triterpenoid compound. It is derived from the hydride of dammarane. Ginsenoside Rb2 has been reported to be found in Gynostemma pentaphyllum, Panax notoginseng, and other organisms with relevant data. See also: Asian ginseng (partial); Panax notoginseng root (partial).
Ginsenoside Rb2 is a major bioactive component of Panax ginseng, one of the most widely used herbal medicines worldwide. It has been extensively studied for its pharmacological activities including antioxidant, anticancer, anti-inflammatory, and antidiabetic effects. Rb2 is not an FDA-approved drug and is intended for research purposes only. It is available from chemical suppliers as a high-purity reference standard. Its multiple mechanisms of action make it a valuable tool for studying ginseng's therapeutic effects. |
| Molecular Formula |
C53H90O22
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|---|---|
| Molecular Weight |
1079.28
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| Exact Mass |
1078.592
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| CAS # |
11021-13-9
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| PubChem CID |
6917976
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
1117.1±65.0 °C at 760 mmHg
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| Melting Point |
197-199ºC
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| Flash Point |
629.4±34.3 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.622
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| LogP |
4.73
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| Hydrogen Bond Donor Count |
14
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| Hydrogen Bond Acceptor Count |
22
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
75
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| Complexity |
1950
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| Defined Atom Stereocenter Count |
29
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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(CC[C@@H]4[C@@]3(CC[C@@H](C4(C)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]([C@H](O6)CO)O)O)O)C)C)O)C)O[C@H]7[C@@H]([C@H]([C@@H]([C@H](O7)CO[C@H]8[C@@H]([C@H]([C@H](CO8)O)O)O)O)O)O)C
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| InChi Key |
NODILNFGTFIURN-GZPRDHCNSA-N
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| InChi Code |
InChI=1S/C53H90O22/c1-23(2)10-9-14-53(8,75-47-43(67)39(63)37(61)29(72-47)22-69-45-41(65)34(58)26(57)21-68-45)24-11-16-52(7)33(24)25(56)18-31-50(5)15-13-32(49(3,4)30(50)12-17-51(31,52)6)73-48-44(40(64)36(60)28(20-55)71-48)74-46-42(66)38(62)35(59)27(19-54)70-46/h10,24-48,54-67H,9,11-22H2,1-8H3/t24-,25+,26-,27+,28+,29+,30-,31+,32-,33-,34-,35+,36+,37+,38-,39-,40-,41+,42+,43+,44+,45-,46-,47-,48-,50-,51+,52+,53-/m0/s1
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| Chemical Name |
(2S,3R,4S,5S,6R)-2-[(2R,3R,4S,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-2-[[(3S,5R,8R,9R,10R,12R,13R,14R,17S)-12-hydroxy-4,4,8,10,14-pentamethyl-17-[(2S)-6-methyl-2-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-[[(2S,3R,4S,5S)-3,4,5-trihydroxyoxan-2-yl]oxymethyl]oxan-2-yl]oxyhept-5-en-2-yl]-2,3,5,6,7,9,11,12,13,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-yl]oxy]oxan-3-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol
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| Synonyms |
NSC 308878; Ginsenoside RB2; Ginsenoside C
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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) |
H2O : ≥ 100 mg/mL (~92.66 mM)
DMSO : ~9.5 mg/mL (~8.80 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.92 mg/mL (0.85 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 9.2 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: ≥ 0.92 mg/mL (0.85 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 9.2 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: ≥ 0.92 mg/mL (0.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (92.66 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9265 mL | 4.6327 mL | 9.2654 mL | |
| 5 mM | 0.1853 mL | 0.9265 mL | 1.8531 mL | |
| 10 mM | 0.0927 mL | 0.4633 mL | 0.9265 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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