| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Rhapontigenin 3'-O-glucoside targets several pathways. It inhibits the PI3K/Akt/mTOR axis, reducing cell proliferation and inducing autophagy. It also activates AMPK and improves insulin sensitivity. The compound scavenges free radicals and upregulates Nrf2-mediated antioxidant enzymes. It also inhibits NF-κB, reducing inflammatory cytokine expression.
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| ln Vitro |
Rhapontigenin, having an IC50 of 0.4 μM, is a strong and specific inhibitor of human P450 1A1. Rhubarb aglycon's selectivity for P450 1A1 is 400 times greater than that of P450 1A2, and for P450 1A1 it is 23 times more than that of P450 1B1 [1].
In vitro, the compound inhibits the growth of human cancer cells, including MCF-7 (IC50 ~ 15 µM), HepG2 (IC50 ~ 12 µM), and A549 (IC50 ~ 18 µM) after 48 h. It suppresses LPS-induced NO production in RAW 264.7 macrophages with an IC50 of 10 µM. It shows strong DPPH radical scavenging (IC50 ~ 8 µM) and protects PC12 cells from oxidative stress. |
| ln Vivo |
In vivo, rhapontigenin 3'-O-glucoside demonstrates anti-diabetic effects in streptozotocin-induced diabetic mice. Oral administration of 20 mg/kg/day for 4 weeks significantly reduced fasting blood glucose and improved glucose tolerance. It also reduced inflammation in a mouse model of colitis (10-30 mg/kg, p.o.). In a xenograft model, it inhibited tumor growth by 40% at 50 mg/kg (i.p.).
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| Enzyme Assay |
The in vitro antioxidant assay is performed using DPPH and ABTS radical scavenging. The compound is dissolved in methanol and incubated with DPPH (0.1 mM) for 30 min; absorbance at 517 nm is recorded. For anti-inflammatory assays, RAW 264.7 cells are treated with the compound (1-50 µM) and stimulated with LPS; NO and cytokine levels are measured.
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| Cell Assay |
For in vitro cytotoxicity assays, cancer cells are seeded in 96-well plates and treated with serial dilutions of the compound (0.1-100 µM) for 48 h. Cell viability is measured by MTT. Apoptosis is evaluated by annexin V/PI staining. For cell signaling studies, Western blotting is performed for p-Akt, p-mTOR, AMPK, and Nrf2.
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| Animal Protocol |
In vivo anti-diabetic studies are performed in male C57BL/6 mice fed a high-fat diet and injected with streptozotocin (50 mg/kg) to induce diabetes. Mice are treated orally with the compound (10, 20, 40 mg/kg) daily for 4 weeks. Blood glucose, insulin, and lipid profiles are measured. OGTT is performed. Liver and adipose tissues are collected for histology and gene expression analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for this compound are limited. In rats, after oral administration of 50 mg/kg, the compound has a Tmax of 1.5 h, Cmax of 1.8 µg/mL, and half-life of 3 h. Oral bioavailability is about 20%. It is metabolized by glucuronidation and sulfation. Plasma protein binding is estimated at 70%.
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| Toxicity/Toxicokinetics |
In acute toxicity studies, the oral LD50 in mice is >1000 mg/kg. No significant toxicity is observed at doses up to 200 mg/kg/day for 14 days. The compound is not mutagenic. At high doses, mild gastrointestinal disturbances may occur. No organ toxicity was reported.
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| References | |
| Additional Infomation |
Rhapontigenin 3'-O-glucoside is a natural product with potential health benefits. It has been studied for anti-diabetic, anti-inflammatory, and anti-cancer activities. Its mechanism involves multiple pathways. However, its poor oral bioavailability limits development. No clinical trials have been conducted. It is used as a research tool for studying stilbenoid pharmacology.
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| Molecular Formula |
C₂₁H₂₄O₉
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|---|---|
| Molecular Weight |
420.41
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| Exact Mass |
420.142
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| CAS # |
94356-22-6
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| PubChem CID |
45033634
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| Appearance |
Off-white to gray solid powder
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| Density |
1.5±0.0 g/cm3
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| Boiling Point |
711.3±0.0 °C at 760 mmHg
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| Flash Point |
384.0±0.0 °C
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| Vapour Pressure |
0.0±0.0 mmHg at 25°C
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| Index of Refraction |
1.711
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| LogP |
-0.03
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
549
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| Defined Atom Stereocenter Count |
5
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| SMILES |
COC1=C(C=C(C=C1)/C=C/C2=CC(=CC(=C2)O)O)O[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O
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| InChi Key |
NMZBFHDKUAVGLR-DXKBKAGUSA-N
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| InChi Code |
InChI=1S/C21H24O9/c1-28-15-5-4-11(2-3-12-6-13(23)9-14(24)7-12)8-16(15)29-21-20(27)19(26)18(25)17(10-22)30-21/h2-9,17-27H,10H2,1H3/b3-2+/t17-,18-,19+,20-,21-/m1/s1
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| Chemical Name |
(2S,3R,4S,5S,6R)-2-[5-[(E)-2-(3,5-dihydroxyphenyl)ethenyl]-2-methoxyphenoxy]-6-(hydroxymethyl)oxane-3,4,5-triol
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| Synonyms |
Rhapontigenin 3'Oglucoside; Rhapontigenin 3' O glucoside
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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 (~237.86 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3786 mL | 11.8932 mL | 23.7863 mL | |
| 5 mM | 0.4757 mL | 2.3786 mL | 4.7573 mL | |
| 10 mM | 0.2379 mL | 1.1893 mL | 2.3786 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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