Rhapontin
Based on 2 publication(s) in Google Scholar
Rhapontin (Rhaponiticin) is an orally aactive SIRT1 agonist and AMPK activator with anti-inflammatory and anti-fibrotic activities. Rhapontin inhibits NLRP3 inflammasome activation by activating SIRT1 and inhibits TGF-β/Smad signaling via the AMPK pathway. Rhapontin reduces intestinal and lung inflammation, inhibits fibroblast differentiation and extracellular matrix deposition, and enhances tight junction protein expression to repair epithelial barriers. Rhapontin can be used in the study of inflammatory bowel diseases (such as ulcerative colitis) and pulmonary fibrosis.
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- Purity: 99.73%
- CAS No.: 155-58-8
- 화학식: C21H24O9
- 분자량:420.41
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Rhapontin
More
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCCLM3 | IC50 |
>100 μM
Compound: 28
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Antiproliferative activity against human HCCLM3 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
Antiproliferative activity against human HCCLM3 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
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[PMID: 34931827] |
| HepG2 | IC50 |
>100 μM
Compound: 28
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Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
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[PMID: 34931827] |
| KB | IC50 |
34 nM
Compound: RHA
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Antitumor activity against FR-positive human KB cells assessed as decrease in cell viability measured after 48 hrs by MTT proliferation assay
Antitumor activity against FR-positive human KB cells assessed as decrease in cell viability measured after 48 hrs by MTT proliferation assay
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[PMID: 23177726] |
Rhapontin (0.4-20 μM; 24 h) inhibits NLRP3 inflammasome activation, reduces IL-1β secretion, and reverses the activation of NF-κB and MAPK signaling pathways by upregulating SIRT1 expression in LPS-stimulated THP-1 macrophages[1].
Rhapontin (0.4-10 μM; 24 h) inhibits NLRP3 inflammasome activation, reduces IL-1β secretion, and reverses the activation of NF-κB and MAPK signaling pathways by upregulating SIRT1 expression in LPS-stimulated THP-1 macrophages[1].
Rhapontin (5-10 μM; 24 h) increases the expression of tight junction proteins ZO-1 and occludin, reduces the Bcl-2/Bax apoptotic protein ratio, and restores epithelial barrier function in NCM460 colon epithelial cells stimulated with TNF-α (10 ng/mL; 6 h)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human intestinal colonic epithelial cells NCM460
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Concentration:0.4 µM, 2 µM, 10 µM
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Incubation Time:24 h
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Result:Significantly reduced the protein levels of NLRP3, cleaved caspase-1, and pro-inflammatory cytokines (IL-1β, TNF-α), while upregulating SIRT1 expression.
Inhibited phosphorylation of NF-κB p65 and MAPKs (ERK, JNK, p38) compared to the LPS-stimulated control group.
Rhapontin (25-100 mg/kg; gavage; once a day; 14 days) significantly reduces lung tissue collagen deposition, inhibits TGF-β/Smad signaling pathway, activates AMPK and downregulates Lox2 and HIF-1α expression, and improves lung function[2] in the Bleomycin (HY-108345)-induced pulmonary fibrosis model in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 female mice (18-22 g, 6-8 weeks old), DSS-induced acute colitis model[1]
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Dosage:100 mg/kg
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Administration:Gavage, once daily for 8 days (days 1-8 post-DSS induction).
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Result:Reduced disease activity index (DAI) score by 35% compared to the DSS group, with significant improvements in body weight loss, diarrhea, and hematochezia.
Histological analysis showed decreased inflammatory cell infiltration (lamina propria and submucosa), reduced crypt damage, and restored colon length.
MPO activity, a marker of neutrophil infiltration, was reduced by 42%.
Western blot showed decreased NLRP3, cleaved caspase-1, and TGF-β1 protein levels, while ZO-1 and occludin expressions were increased by 58% and 45%, respectively.
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Animal Model:C57BL/6 male mice (20-22 g, 6-8 weeks old) with Bleomycin (HY-108345)-induced pulmonary fibrosis model[2]
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Dosage:25, 50, 100 mg/kg; Prednisone (6.5 mg/kg, positive control).
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Administration:Gavage, once daily for 14 days (days 7-21 post-bleomycin instillation).
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Result:At 100 mg/kg, reduced pulmonary index (lung weight/body weight) by 28% compared to the model group, with decreased collagen deposition.
Reduced TGF-β1, α-SMA, and Lox2 protein expressions by 41%, 37%, and 53%, respectively, while AMPK phosphorylation (p-AMPK/AMPK ratio) was increased by 62%.
ELISA showed decreased BALF levels of IL-1β.
Chemical Information
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CAS No. 155-58-8
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Appearance Solid
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분자량 420.41
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화학식 C21H24O9
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Color Off-white to yellow
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SMILES
O[C@H]([C@@H](O)[C@@H]1O)[C@@H](O[C@@H]1CO)OC2=CC(/C=C/C3=CC(O)=C(OC)C=C3)=CC(O)=C2
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Synonyms
Rhaponiticin
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Structure Classification
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Initial Source
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (2)
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Journal Impact Factor
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Most Recent
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Redox Biol
Gaylussacin, a stilbene glycoside, inhibits chronic obstructive pulmonary disease in mice. [Abstract]2025 Jun 26:85:103744. PMID: 40614364 -
Biomed Res Int
Anti-influenza A Virus Effects and Mechanisms of Emodin and Its Analogs via Regulating PPAR α/ γ-AMPK-SIRT1 Pathway and Fatty Acid Metabolism. [Abstract]2021 Sep 9;2021:9066938. PMID: 34540999
용액&용해도
DMSO : 250 mg/mL (594.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (279 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Wei W, et al. Rhapontin ameliorates colonic epithelial dysfunction in experimental colitis through SIRT1 signaling. Int Immunopharmacol. 2017 Jan;42:185-194. [Content Brief]
[2]. Tao L, et al. Protective role of rhapontin in experimental pulmonary fibrosis in vitro and in vivo. Int Immunopharmacol. 2017 Jun;47:38-46. [Content Brief]
[3]. Hibasami H, et al. Induction of apoptosis by rhapontin having stilbene moiety, a component of rhubarb (Rheum officinale Baillon) in human stomach cancer KATO III cells. Oncol Rep. 2007 Aug;18(2):347-51. [Content Brief]
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 (protect from light). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3786 mL | 11.8932 mL | 23.7863 mL | 59.4658 mL |
| 5 mM | 0.4757 mL | 2.3786 mL | 4.7573 mL | 11.8932 mL | |
| 10 mM | 0.2379 mL | 1.1893 mL | 2.3786 mL | 5.9466 mL | |
| 15 mM | 0.1586 mL | 0.7929 mL | 1.5858 mL | 3.9644 mL | |
| 20 mM | 0.1189 mL | 0.5947 mL | 1.1893 mL | 2.9733 mL | |
| 25 mM | 0.0951 mL | 0.4757 mL | 0.9515 mL | 2.3786 mL | |
| 30 mM | 0.0793 mL | 0.3964 mL | 0.7929 mL | 1.9822 mL | |
| 40 mM | 0.0595 mL | 0.2973 mL | 0.5947 mL | 1.4866 mL | |
| 50 mM | 0.0476 mL | 0.2379 mL | 0.4757 mL | 1.1893 mL | |
| 60 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9911 mL | |
| 80 mM | 0.0297 mL | 0.1487 mL | 0.2973 mL | 0.7433 mL | |
| 100 mM | 0.0238 mL | 0.1189 mL | 0.2379 mL | 0.5947 mL |
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