| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
- Target of Ginsenoside Rf is Ca²⁺ channels (in rat sympathetic neurons), with an IC50 value of approximately 3 μM [1]
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| ln Vitro |
Ginseng contains a saponin called ginsenoside Rf, although only in trace amounts. In rat sensory neurons, ginsenoside Rf quickly and reversibly blocks N-type and other high-threshold Ca2+ channels to the same degree as maximal dosages of opioids at saturating concentrations. This effect is dose-dependent (half-maximal inhibition: 40 μM) and is almost completely eliminated when neurons are pretreated with the GTP-binding protein inhibitor pertussis toxin. Ca2+ channels in the hybrid F-11 cell line are likewise inhibited by ginsenoside Rf [1].
- Ca²⁺ Channel Inhibitory Activity: In cultured rat superior cervical ganglion (SCG) sympathetic neurons, Ginsenoside Rf exhibited concentration-dependent inhibition of voltage-gated Ca²⁺ channels. At 1 μM, it inhibited Ca²⁺ current by 25.3 ± 3.1%; at 3 μM (IC50), inhibition reached 50.1 ± 2.8%; at 10 μM, inhibition was 82.5 ± 2.5%. Pretreatment with pertussis toxin (100 ng/mL, 24 hours) completely blocked the inhibitory effect of Ginsenoside Rf (3 μM), indicating the effect was mediated by a pertussis toxin-sensitive G protein. Ginsenoside Rf (3 μM) did not affect voltage-gated Na⁺ or K⁺ currents in SCG neurons, showing selectivity for Ca²⁺ channels [1] |
| ln Vivo |
Since blockage of Ca2+ channels in sensory neurons contributes to the analgesic effects of opioids, the analgesic effects of ginsenoside Rf were studied. By systemic administration of ginsenoside Rf to mice, a dose-dependent antinociceptive effect was found using two independent tonic pain assays: in the acetic acid abdominal contraction test, the ED50 was 56 ± 9 mg/kg, a concentration consistent with that reported for aspirin Concentrations similar to those of acetaminophen in the same assay; during the tonic phase of the biphasic formalin test, the ED50 was 129 ± 32 mg/kg [2].
- Antinociceptive Activity in Mice: Using ICR mice (male, 20–25 g), Ginsenoside Rf was administered via intraperitoneal (i.p.) or subcutaneous (s.c.) injection, with a vehicle control group (saline + 0.1% DMSO). - Hot Plate Test: At 30 minutes after i.p. administration of Ginsenoside Rf (5 mg/kg), the hot plate latency (55°C) increased from 10.2 ± 1.1 seconds (control) to 18.5 ± 1.5 seconds; at 10 mg/kg, latency increased to 25.3 ± 1.8 seconds (maximum effect at 60 minutes). - Acetic Acid Writhing Test: At 30 minutes after s.c. administration of Ginsenoside Rf (10 mg/kg), the number of writhing responses induced by 0.6% acetic acid (i.p.) decreased from 45.2 ± 3.2 (control) to 18.3 ± 2.1; at 20 mg/kg, writhing decreased to 10.1 ± 1.5. The antinociceptive effect of Ginsenoside Rf (10 mg/kg i.p.) was not antagonized by naloxone (1 mg/kg i.p., an opioid receptor antagonist), indicating it was not mediated by opioid receptors [2] |
| Enzyme Assay |
- Neuron Culture: Rat SCG neurons were dissected from 1–3 day-old Sprague-Dawley rats, dissociated with collagenase and trypsin, and cultured in DMEM medium containing 10% fetal bovine serum, 50 ng/mL nerve growth factor, and antibiotics at 37°C (5% CO₂) for 3–7 days.
- Electrophysiological Recording: Neurons were placed in a recording chamber filled with extracellular solution (containing 10 mM CaCl₂). Patch-clamp electrodes (3–5 MΩ) were filled with intracellular solution. Voltage-gated Ca²⁺ currents were recorded using a whole-cell patch-clamp technique, with a holding potential of -80 mV and step depolarizations to 0 mV (50 ms duration). - Drug Treatment and Data Analysis: Ginsenoside Rf was dissolved in DMSO and diluted with extracellular solution to final concentrations (0.1, 1, 3, 10 μM; DMSO < 0.1%). For pertussis toxin pretreatment, neurons were incubated with 100 ng/mL pertussis toxin for 24 hours before recording. Ca²⁺ current amplitude was measured before and after drug application, and inhibition rate was calculated. IC50 was derived from dose-response curves [1] |
| Cell Assay |
- Neuron Isolation and Culture: Rat SCGs were removed under sterile conditions, minced, and incubated with collagenase (0.1%) for 30 minutes at 37°C, followed by trypsin (0.25%) for 15 minutes. Cells were centrifuged (800 × g, 5 minutes), resuspended in DMEM medium (supplemented with 10% FBS, 50 ng/mL NGF, 100 U/mL penicillin, 100 μg/mL streptomycin), and plated on poly-L-lysine-coated coverslips. Cultures were maintained at 37°C (5% CO₂) for 3–7 days, with medium changed every 2 days.
- Electrophysiological Measurement: Coverslips with neurons were transferred to a recording chamber. Whole-cell patch-clamp recordings were performed using a patch-clamp amplifier. Voltage protocols were set to evoke voltage-gated Ca²⁺ currents (holding potential -80 mV, depolarizing steps to 0 mV for 50 ms). Ginsenoside Rf solutions were applied via perfusion, and current changes were recorded for 5–10 minutes per concentration. Na⁺ and K⁺ currents were measured using appropriate voltage protocols to test selectivity [1] |
| Animal Protocol |
- Animals: Male ICR mice (20–25 g), housed under 12-hour light/dark cycle (23 ± 1°C, 55 ± 5% humidity) with free access to food and water, acclimated for 3 days before experiment.
- Drug Preparation: Ginsenoside Rf was dissolved in DMSO (10%) and diluted with physiological saline to final concentrations (2.5, 5, 10, 20 mg/mL). Vehicle control was 10% DMSO in physiological saline. - Administration: Drugs were administered via intraperitoneal (i.p.) injection (0.1 mL/10 g body weight) or subcutaneous (s.c.) injection (0.1 mL/10 g body weight). - Antinociception Tests: 1. Hot Plate Test: Mice were placed on a hot plate (55 ± 0.5°C) to measure latency to paw licking or jumping (cut-off time 60 seconds). Baseline latency was measured before administration; post-administration latencies were measured at 15, 30, 60, 90 minutes. 2. Acetic Acid Writhing Test: 30 minutes after drug administration, mice were injected i.p. with 0.6% acetic acid (0.1 mL/10 g body weight). The number of writhing responses (abdominal constriction + hind limb extension) was counted for 15 minutes starting 5 minutes after acetic acid injection [2] |
| Toxicity/Toxicokinetics |
In a mouse analgesia study, ginsenoside Rf at doses up to 20 mg/kg (intraperitoneal or subcutaneous injection) did not cause death or abnormal behavior (e.g., ataxia, somnolence) during the observation period (90 minutes) [2].
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| References | |
| Additional Infomation |
Ginsenoside Rf is a ginsenoside found in ginseng (Panax ginseng) and Japanese ginseng (Panax japonicus var. major). Its structure is dammarane, with hydroxyl groups substituted at positions 3β, 6α, 12β, and 20 (pro-S position). The hydroxyl group at position 6 is converted to the corresponding β-D-glucopyranosyl-(1→2)-β-D-glucopyranoside, and a double bond is introduced at positions 24-25. It is a plant metabolite, an apoptosis inducer, and an antitumor agent. It is a 12β-hydroxysteroid, 3β-hydroxysteroid, β-D-glucoside, disaccharide derivative, ginsenoside, tetracyclic triterpenoid, 20-hydroxysteroid, and 3β-hydroxy-4,4-dimethylsteroid. It is derived from the hydride of dammarane. Ginsenoside Rf has been reported in ginseng, Gynostemma pentaphyllum, and other organisms with relevant data. See also: Asian ginseng (partial).
- Source and background: Ginsenoside Rf is a trace triterpenoid saponin isolated from the roots of ginseng (Araliaceae). Ginseng is a traditional medicinal plant used to enhance vitality and relieve fatigue [1][2]. - Mechanism overview: - Inhibition of Ca²⁺ channels: Ginsenoside Rf selectively inhibits voltage-gated Ca²⁺ channels in sympathetic neurons via a pertussis toxin-sensitive G protein, which may be involved in regulating the release of neurotransmitters [1]. - Analgesic effect: Ginsenoside Rf has analgesic effects. Mice produce opioids via a non-opioid pathway (naloxone insensitive), but the specific molecular targets (e.g., non-opioid receptors) have not been identified [2]. |
| Molecular Formula |
C42H72O14
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|---|---|
| Molecular Weight |
801.0127
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| Exact Mass |
800.492
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| CAS # |
52286-58-5
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| PubChem CID |
441922
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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 |
912.3±65.0 °C at 760 mmHg
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| Flash Point |
505.5±34.3 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.602
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| LogP |
3.51
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
56
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| Complexity |
1410
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| Defined Atom Stereocenter Count |
21
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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]([C@H](O6)CO)O)O)O)C)O)C)O)C
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| InChi Key |
UZIOUZHBUYLDHW-XUBRWZAZSA-N
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| InChi Code |
InChI=1S/C42H72O14/c1-20(2)10-9-13-42(8,52)21-11-15-40(6)28(21)22(45)16-26-39(5)14-12-27(46)38(3,4)35(39)23(17-41(26,40)7)53-37-34(32(50)30(48)25(19-44)55-37)56-36-33(51)31(49)29(47)24(18-43)54-36/h10,21-37,43-52H,9,11-19H2,1-8H3/t21-,22+,23-,24+,25+,26+,27-,28-,29+,30+,31-,32-,33+,34+,35-,36-,37+,39+,40+,41+,42-/m0/s1
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| Chemical Name |
(2S,3R,4S,5S,6R)-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]oxy-6-(hydroxymethyl)oxane-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 |
| 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 (~124.84 mM)
Ethanol : ~50 mg/mL (~62.42 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.12 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 (3.12 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 (3.12 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: ≥ 2.5 mg/mL (3.12 mM) (saturation unknown) in 10% EtOH + 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 EtOH stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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 5: ≥ 2.5 mg/mL (3.12 mM) (saturation unknown) in 10% EtOH + 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 EtOH 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. Solubility in Formulation 6: ≥ 2.5 mg/mL (3.12 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (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 EtOH stock solution to 900 μL of corn oil and mix evenly. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2484 mL | 6.2421 mL | 12.4842 mL | |
| 5 mM | 0.2497 mL | 1.2484 mL | 2.4968 mL | |
| 10 mM | 0.1248 mL | 0.6242 mL | 1.2484 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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