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Ginsenoside Rb1

Cat No.:V21594 Purity: ≥98%
Ginsenoside Rb1 is a component of the traditional Chinese medicine ginseng.
Ginsenoside Rb1
Ginsenoside Rb1 Chemical Structure CAS No.: 41753-43-9
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
Ginsenoside Rb1 is a component of the traditional Chinese medicine ginseng. Ginsenoside inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside Rb1 also inhibits IRAK-1 activation and NF-κB p65 phosphorylation.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
Ginsenoside Rb1's IC50 against Na+ and K+-ATPase is 6.3±1.0 μM. Simultaneously, ginsenoside is a non-competitive ATP coupling, as demonstrated by the kinetic analysis of the rise in ginsenoside Rb1 concentration or the increase in Na+ and K+ concentration [1]. The reduction of IKK-β and IRAK-1 receptor-associated pump 1 (IRAK-1) was significantly inhibited by ginsenoside Rb1, which also improved the inhibitory effect. MAP moieties (ERK, JNK, and p-38) and NF-κB activation; however, no connection has been found between LPS and Toll-like receptor 4 responses, IRAK-2 activation, or IRAK-4 activation [2]. Rb1 is a part of ginseng, a traditional Chinese medicine. The primary bioactive ingredient that controls pro-alkane X receptor (PXR)/NF-κB signaling is ginsenoside Rb1. Ginsenoside Rb1 in ginsenoside extract (GSE) exhibits strong anti-inflammatory properties. Based on preliminary studies, the concentration of ginsenoside Rb1 (10 μM) in cells was optimized to ensure adequate anti-inflammatory activity without evident toxicity. Ginsenoside Rb1 returned the mRNA levels of PXR and CYP3A4 to LS174T cells and significantly decreased the TNF-α-induced upregulation of IL-1β and iNOS. Ginsenoside Rb1 significantly eliminated both the significant increase in the ratio of phosphorylated to total NF-κB p65 and the significant decrease in PXR protein levels caused by TNF-α [3].
ln Vivo
Ginsenoside Rb1, at doses of 30 mg/kg and 60 mg/kg, significantly reduced lung damage as shown by histology. In older adults, ginsenoside Rb1 at 30 mg/kg and 60 mg/kg significantly reduced histological lung damage [4]. Rb1) has a positive impact on the underlying mechanism of intestinal membrane microvascular wafer permeability generated by lipopolysaccharide (LPS) and is a constituent of the traditional Chinese medication ginseng. Thirty minutes after cosmetic LPS infusion, ginsenoside Rb1 (5 mg/kg) flowed via the left jugular system in certain stents. Within microvessels, ginsenoside Rb1 decreases the amount of caveolae in the cell skin. Due to its capacity to suppress NF-κB and Src activation, ginsenoside Rb1 improves microvascular hyperpermeability following endotoxin demand and eliminates intestinal edema by decreasing development of caveolae and connections [5].
References

[1]. Inhibitory effects of ginsenoside Rg1 and Rb1 on rat brain microsomal Na+,K+-ATPase activity. Zhongguo Yao Li Xue Bao. 1990 Jan;11(1):10-4.

[2]. Ginsenosides Regulate PXR/NF-κB Signaling and Attenuate Dextran Sulfate Sodium-Induced Colitis. Drug Metab Dispos. 2015 Aug;43(8):1181-9.

[3]. Ginsenoside Rb1 and its metabolite compound K inhibit IRAK-1 activation--the key step of inflammation. Biochem Pharmacol. 2011 Aug 1;82(3):278-86.

[4]. Ginsenoside Rb1 Treatment Attenuates Pulmonary Inflammatory Cytokine Release and Tissue Injury following Intestinal Ischemia Reperfusion Injury in Mice. Oxid Med Cell Longev. 2015;2015:843721.

[5]. Ginsenoside Rb1 ameliorates lipopolysaccharide-induced albumin leakage from rat mesenteric venules by intervening in both trans- and paracellular pathway. Am J Physiol Gastrointest Liver Physiol. 2014 Feb 15;306(4):G289-300.

Additional Infomation
Ginsenoside Rb1 is a ginsenoside found in Panax ginseng and Panax japonicus var. major that is ginsenoside Rd in which the beta-D-glucopyranoside group at position 20 is replaced by a beta-D-glucopyranosyl-beta-D-glucopyranoside group. It has a role as a neuroprotective agent, an anti-obesity agent, an anti-inflammatory drug, an apoptosis inhibitor, a radical scavenger and a plant metabolite. It is a ginsenoside, a glycoside and a tetracyclic triterpenoid. It is functionally related to a ginsenoside Rd.
Ginsenosides are a class of steroid glycosides, and triterpene saponins, found exclusively in the plant genus Panax (ginseng). Ginsenosides have been the target of research, as they are viewed as the active compounds behind the claims of ginseng's efficacy. Because ginsenosides appear to affect multiple pathways, their effects are complex and difficult to isolate. Rb1 appears to be most abundant in Panax quinquefolius (American Ginseng). Rb1 seems to affect the reproductive system in animal testicles. Recent research shows that Rb1 affects rat embryo development and has teratogenic effects, causing birth defects. Another study shows that Rb1 may increase testosterone production in male rats indirectly through the stimulation of the luteinizing hormone.
Ginsenoside rb1 has been reported in Panax japonicus, Glycyrrhiza uralensis, and other organisms with data available.
See also: American Ginseng (part of); Asian Ginseng (part of); Panax notoginseng root (part of).
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C54H92O23
Molecular Weight
1109.2945
Exact Mass
1108.602
CAS #
41753-43-9
PubChem CID
9898279
Appearance
White to off-white solid powder
Density
1.4±0.1 g/cm3
Boiling Point
1145.9±65.0 °C at 760 mmHg
Flash Point
646.8±34.3 °C
Vapour Pressure
0.0±0.6 mmHg at 25°C
Index of Refraction
1.626
LogP
2.9
Hydrogen Bond Donor Count
15
Hydrogen Bond Acceptor Count
23
Rotatable Bond Count
16
Heavy Atom Count
77
Complexity
2000
Defined Atom Stereocenter Count
30
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]([C@H](O8)CO)O)O)O)O)O)O)C
InChi Key
GZYPWOGIYAIIPV-JBDTYSNRSA-N
InChi Code
InChI=1S/C54H92O23/c1-23(2)10-9-14-54(8,77-48-44(69)40(65)37(62)29(74-48)22-70-46-42(67)38(63)34(59)26(19-55)71-46)24-11-16-53(7)33(24)25(58)18-31-51(5)15-13-32(50(3,4)30(51)12-17-52(31,53)6)75-49-45(41(66)36(61)28(21-57)73-49)76-47-43(68)39(64)35(60)27(20-56)72-47/h10,24-49,55-69H,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-,49-,51-,52+,53+,54-/m0/s1
Chemical Name
(2R,3R,4S,5S,6R)-2-[[(2R,3S,4S,5R,6S)-6-[(2S)-2-[(3S,5R,8R,9R,10R,12R,13R,14R,17S)-3-[(2R,3R,4S,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-3-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-12-hydroxy-4,4,8,10,14-pentamethyl-2,3,5,6,7,9,11,12,13,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]-6-methylhept-5-en-2-yl]oxy-3,4,5-trihydroxyoxan-2-yl]methoxy]-6-(hydroxymethyl)oxane-3,4,5-triol
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~90.15 mM)
H2O : ≥ 33.33 mg/mL (~30.05 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.25 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 (2.25 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.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (2.25 mM) (saturation unknown) in 10% DMSO + 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 DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.9015 mL 4.5073 mL 9.0147 mL
5 mM 0.1803 mL 0.9015 mL 1.8029 mL
10 mM 0.0901 mL 0.4507 mL 0.9015 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.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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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