1. Membrane Transporter/Ion Channel Immunology/Inflammation NF-κB Autophagy Anti-infection
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  3. Ginsenoside Rb1

Ginsenoside Rb1  (Synonyms: Gypenoside III)

Cat. No.: HY-N0039 Purity: 98.75%
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Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with an IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 .

For research use only. We do not sell to patients.

Ginsenoside Rb1 Chemical Structure

Ginsenoside Rb1 Chemical Structure

CAS No. : 41753-43-9

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Customer Review

Based on 6 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with an IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 .

IC50 & Target[1][2][3][6]

Na+, K+-ATPase

6.3 μM (IC50)

IRAK-1

 

p65

 

Autophagy

 

Mitophagy

 

HSV-1

 

In Vitro

Rat brain microsomal Na+, K+-ATPase activity is inhibited significantly and rapidly by Ginsenoside Rb1. The IC50 of Ginsenoside Rb1 for Na+,K+-ATPase is 6.3±1.0 μM. The inhibition is enhanced with increasing the concentration of Ginsenoside Rb1 or decreasing that of Na+ and K+. Kinetic analysis reveals that Ginsenoside is an uncompetitive inhibitor with respect to ATP[1]. Ginsenoside Rb1 significantly inhibits the activation of interleukin-1 receptor-associated kinase-1 (IRAK-1), IKK-β, NF-κB, and MAP kinases (ERK, JNK, and p-38); however, interaction between LPS and Toll-like receptor-4, IRAK-4 activation and IRAK-2 activation are unaffected[2]. Ginsenoside Rb1 is an ingredient of a Chinese medicine Panax ginseng. Ginsenoside Rb1 is a major bioactive compound in the regulating pregnane X receptor (PXR)/NF-κB signaling. Ginsenoside Rb1 is the compound with potent anti-inflammatory activity in ginseng saponin extract (GSE). The concentration for Ginsenoside Rb1 (10 μM) is optimized from a preliminary study to ensure sufficient anti-inflammatory activity and without apparent cytotoxicity. Ginsenoside Rb1 significantly reduces TNF-α-induced upregulation of IL-1β and iNOS mRNA levels, and restores the mRNA levels of PXR and CYP3A4 in LS174T cells. TNF-α causes a significant reduction in PXR protein levels and increase in the ratio of phosphorylated to total NF-κB p65, both of which are significantly abrogated by Ginsenoside Rb1[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ginsenoside Rb1 at the both doses of 30 mg/kg and 60 mg/kg significantly attenuates the histological lung injury. Ginsenoside Rb1 at the dose of 30 mg/kg and 60 mg/kg both significantly attenuates the histological intestine injury[4]. Ginsenoside Rb1 (Rb1), an ingredient of a Chinese medicine Panax ginseng, has beneficial effects on mesentery microvascular hyperpermeability induced by Lipopolysaccharide (LPS) and the underlying mechanisms. In some rats, Ginsenoside Rb1 (5 mg/kg per hour) is administrated through the left jugular vein 30 min after LPS infusion. Ginsenoside Rb1 decreases caveolae number in endothelial cells of microvessels. Ginsenoside Rb1 ameliorates microvascular hyperpermeability after the onset of endotoxemia and improves intestinal edema through inhibiting caveolae formation and junction disruption, which is correlated to suppression of NF-κB and Src activation[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

1109.29

Formula

C54H92O23

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]([C@@]12C)(CC[C@@]3([H])C4(C)C)[C@@](C[C@@H](O)[C@]1([H])[C@]([C@@](CC/C=C(C)/C)(C)O[C@@H]([C@@H]([C@@H](O)[C@@H]5O)O)O[C@@H]5CO[C@@H]([C@@H]([C@@H](O)[C@@H]6O)O)O[C@@H]6CO)([H])CC2)([H])[C@]3(CC[C@@H]4O[C@@](O[C@H](CO)[C@@H](O)[C@@H]7O)([H])[C@@H]7O[C@]([C@@H]([C@@H](O)[C@@H]8O)O)([H])O[C@@H]8CO)C

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (90.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 33.33 mg/mL (30.05 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9015 mL 4.5074 mL 9.0148 mL
5 mM 0.1803 mL 0.9015 mL 1.8030 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 98.75%

References
Cell Assay
[3]

LS174T cells are seeded in cell imaging dish. After overnight incubation, cells are treated with GSE (100 μg/mL), Ginsenoside Rb1 (10 μM), or CK (10 μM) for 3 hours, followed by an additional incubation with or without TNF-α (20 ng/ml) for 6 hours. At the end of the incubation, cells are harvested and fixed with 4% paraformaldehyde solution at 20°C for 20 minutes. After washing in PBS, cells are permeabilized with 0.2% Triton X-100 in PBS at room temperature for 5 minutes. After incubation in blocking buffer containing 0.1% Triton X-100 and 5% bovine serum albumin, cells are incubated with rabbit NF-κB p65 antibody at 4°C overnight and then with Alexa Fluor 488-conjugated anti-rabbit IgG antibody at room temperature for 30 minutes in 1% bovine serum albumin in PBS. Fluorescence photographs are obtained using a Zeiss 710 confocal microscope[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4][5]

Mice[4]
Male C57BL/6 mice (9-12 weeks old; 17-22 g) are randomly allocated into eight groups (n=8 in each group): (1) Sham surgical preparation including isolation of the superior mesenteric artery (SMA) without occlusion is performed (Sham); (2) mice are subjected to II/R without treatment (II/R); (3) mice are subjected to II/R with treatment of normal saline 10 minutes before reperfusion (II/R+NS); (4), (5) mice are treated with 30 mg/kg (II/R+Rb1-30) or 60 mg/kg (II/R+Rb1-60) Ginsenoside Rb1, in which surgery is performed as in the II/R group with administration of the Ginsenoside Rb1 intraperitoneally 10 minutes before reperfusion; (6) mice are subjected to Sham surgery and treated with ATRA (ATRA+Sham), which is the inhibitor of Nrf2/ARE signaling pathway; (7) mice are subjected to II/R and treated with ATRA (ATRA+II/R); (8) mice are subjected to II/R and treated with ATRA and 60 mg/kg Ginsenoside Rb1 as group 5 (ATRA+II/R+Rb1-60). During the last two weeks before the operation, the mice in the group 6, 7, 8 receive ATRA i.p. daily at 10 mg/kg and fed on a vitamin A-deficient diet, and the mice in the other groups receive the equivalent volume of corn oil and fed on a control normal diet.
Rats[5]
Male Wistar rats weighing 200-250 g are used. The rats are randomly divided into four groups, 26 animals in each. After being anesthetized with urethane (2 g/kg body wt im), the left femoral vein and left jugular vein of the rat are cannulated. In the LPS group, LPS solution in saline is infused (5 mg/kg per hour) for 90 min via the left femoral vein. The vehicle, instead of LPS solution, is administrated in Sham and Ginsenoside Rb1 alone (Rb1, 5 mg/kg) groups. In the Rb1 posttreatment (LPS+Rb1) group, Ginsenoside Rb1 solution is infused continuously through the left jugular vein 30 min after LPS administration at the dose of 5 mg/kg. Ginsenoside Rb1 solution and the same volume of saline are infused in Ginsenoside Rb1 and Sham groups, respectively, without subsequent LPS administration. In a separate set of experiments, the rats are anesthetized with 2% penobarbital sodium (60 mg/kg body wt ip), and saline, LPS, and Ginsenoside Rb1. After recovery from anesthesia, the animals are allowed access to water and rodent chow, and survival rate is recorded over time until 4 days after LPS stimulation.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 0.9015 mL 4.5074 mL 9.0148 mL 22.5369 mL
5 mM 0.1803 mL 0.9015 mL 1.8030 mL 4.5074 mL
10 mM 0.0901 mL 0.4507 mL 0.9015 mL 2.2537 mL
15 mM 0.0601 mL 0.3005 mL 0.6010 mL 1.5025 mL
20 mM 0.0451 mL 0.2254 mL 0.4507 mL 1.1268 mL
25 mM 0.0361 mL 0.1803 mL 0.3606 mL 0.9015 mL
30 mM 0.0300 mL 0.1502 mL 0.3005 mL 0.7512 mL
DMSO 40 mM 0.0225 mL 0.1127 mL 0.2254 mL 0.5634 mL
50 mM 0.0180 mL 0.0901 mL 0.1803 mL 0.4507 mL
60 mM 0.0150 mL 0.0751 mL 0.1502 mL 0.3756 mL
80 mM 0.0113 mL 0.0563 mL 0.1127 mL 0.2817 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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