Rhapontigenin
Based on 3 publication(s) in Google Scholar
Rhapontigenin is a natural analog of resveratrol with anticancer, antioxidant, antifungal and antibacterial activities. Rhapontigenin is amechanism-based, potent and selective cytochrome P450 1A1 inactivator (IC50 = 400 nM). Rhapontigenin exhibits 400-fold and 23-fold selectivity for P450 1A1 over P450 1A2 and P450 1B1, respectively.
For research use only. We do not sell to patients.
- Purity: 99.66%
- CAS No.: 500-65-2
- Formula: C15H14O4
- Molecular Weight:258.27
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Rhapontigenin
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Customer Validation & Images
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Histological Imaging/Staining
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WB
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IF
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RT-PCR
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IHC
Biological Activity
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CYP1A1 400 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HL-60 | IC50 |
48 μM
Compound: 10a
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In vitro inhibitory concentration against proliferation of HL60 cells
In vitro inhibitory concentration against proliferation of HL60 cells
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[PMID: 12877593] |
| J774 | IC50 |
102.8 μM
Compound: 6
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Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced nitric oxide production after 24 hrs by Griess assay
Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced nitric oxide production after 24 hrs by Griess assay
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[PMID: 29726680] |
| J774 | IC50 |
19.4 μM
Compound: 6
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Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced MCP1 expression after 24 hrs by ELISA
Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced MCP1 expression after 24 hrs by ELISA
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[PMID: 29726680] |
| J774 | IC50 |
99.1 μM
Compound: 6
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Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced IL6 expression after 24 hrs by ELISA
Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced IL6 expression after 24 hrs by ELISA
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[PMID: 29726680] |
Rhapontigenin (0-250 μM; 24 hours) demonstrates concentration-dependent?anti-cancer?activity with an IC50 115μM in HEP G2 cells[1].? Rhapontigenin (20 μM; 20 hours) pre-treatment decreases TGF-β triggered increased snail expression in diverse cancer cells[2].? Rhapontigenin (0-20 μM; 6 hours) inhibits TGF-β-induced expression of N-cadherin, vimentin, and CA9 in a dose-dependent manner[2].? Rhapontigenin inhibits ADP- and collagen-induced platelet aggregation with IC50 values of 4 and 70 μg/ml, respectively[3].? Rhapontigenin demonstrates a strong inhibitory activity on the 13-hexosaminidase release induced by DNP-BSA, it exhibits IC50 value of 0.03 mM in RBL 2H3 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa, A549,769-P cells
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Concentration:0 μM; 2.5 μM; 5 μM; 10 μM; 20 μM
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Incubation Time:6 hours
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Result:Induced ubiquitination and degradation of HIF-1α.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice[3]
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Dosage:25mg/kg
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Administration:25mg/kg; intraperitoneal injection
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Result:Showed anti-thrombosis activity with 60% protection.
Chemical Information
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CAS No. 500-65-2
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Appearance Solid
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Molecular Weight 258.27
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Formula C15H14O4
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Color Light yellow to yellow
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SMILES
OC1=CC(/C=C/C2=CC=C(OC)C(O)=C2)=CC(O)=C1
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Biomed Eng
Amelioration of Alzheimer's disease pathology by mitophagy inducers identified via machine learning and a cross-species workflow. [Abstract]2022 Jan;6(1):76-93. PMID: 34992270
Rhapontigenin purchased from MedChemExpress. Usage Cited in: Nat Biomed Eng. 2022 Jan;6(1):76-93. [Abstract]
Effects of Kaem and Rhapontigenin (Rhap) (20, 40, 80 μM) on the protein levels of mitofusin2 (MFN2), YFP-Parkin and Tim23 in HeLa cells stably overexpressing YFP-Parkin.
Rhapontigenin purchased from MedChemExpress. Usage Cited in: Nat Biomed Eng. 2022 Jan;6(1):76-93. [Abstract]
Images showing co-localization of mitochondria (Mito-GFP) and lysosomes (LAMP1 antibody) under Kaem and Rhapontigenin (Rhap) (20 uM, 24 h) administration in GFP-mito-mCherry-Parkin HeLa cells.
Rhapontigenin purchased from MedChemExpress. Usage Cited in: Nat Biomed Eng. 2022 Jan;6(1):76-93. [Abstract]
Effects of Kaem and Rhapontigenin (Rhap) (0.2 mM) on designated gene expression in day 1 adult worms.
Rhapontigenin purchased from MedChemExpress. Usage Cited in: Nat Biomed Eng. 2022 Jan;6(1):76-93. [Abstract]
Immunohistochemical analysis of Aβ load in 3xTg AD mice hippocampi and cortices under Kaem or Rhapontigenin (Rhap) (100 mg/kg, p.o.) treatment.
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Int Immunopharmacol
Rhapontigenin inhibits inflammation and senescence of chondrocytes from patients with osteoarthritis by targeting INHBA. [Abstract]2026 Jan 1;168(Pt 1):115808. PMID: 41218586 -
FASEB J
Epigenetic mechanisms mediate cytochrome P450 1A1 expression and lung endothelial injury caused by MRSA in vitro and in vivo. [Abstract]2024 Nov 30;38(22):e70205. PMID: 39588951
Rhapontigenin purchased from MedChemExpress. Usage Cited in: FASEB J. 2024 Nov 30;38(22):e70205. [Abstract]
Lung tissue H&E staining treated with Rhapontigenin (Rhap) (10 mg/kg, i.p.).
Solvent & Solubility
DMSO : 125 mg/mL (483.99 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 (8.05 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 (8.05 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.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Roupe KA, et al. Preparative enzymatic synthesis and HPLC analysis of rhapontigenin: applications to metabolism, pharmacokinetics and anti-cancer studies.J Pharm Pharm Sci. 2005 Aug 22;8(3):374-86. [Content Brief]
[2]. Yeh YH, et al. Rhapontigenin inhibits TGF-β-mediated epithelial‑mesenchymal transition via the PI3K/AKT/mTOR pathway and is not associated with HIF-1α degradation.Oncol Rep. 2016 May;35(5):2887-95. [Content Brief]
[3]. Park EK, et al. Antithrombotic and antiallergic activities of rhaponticin from Rhei Rhizoma are activated by human intestinal bacteria.Arch Pharm Res. 2002 Aug;25(4):528-33. [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 | 3.8719 mL | 19.3596 mL | 38.7192 mL | 96.7979 mL |
| 5 mM | 0.7744 mL | 3.8719 mL | 7.7438 mL | 19.3596 mL | |
| 10 mM | 0.3872 mL | 1.9360 mL | 3.8719 mL | 9.6798 mL | |
| 15 mM | 0.2581 mL | 1.2906 mL | 2.5813 mL | 6.4532 mL | |
| 20 mM | 0.1936 mL | 0.9680 mL | 1.9360 mL | 4.8399 mL | |
| 25 mM | 0.1549 mL | 0.7744 mL | 1.5488 mL | 3.8719 mL | |
| 30 mM | 0.1291 mL | 0.6453 mL | 1.2906 mL | 3.2266 mL | |
| 40 mM | 0.0968 mL | 0.4840 mL | 0.9680 mL | 2.4199 mL | |
| 50 mM | 0.0774 mL | 0.3872 mL | 0.7744 mL | 1.9360 mL | |
| 60 mM | 0.0645 mL | 0.3227 mL | 0.6453 mL | 1.6133 mL | |
| 80 mM | 0.0484 mL | 0.2420 mL | 0.4840 mL | 1.2100 mL | |
| 100 mM | 0.0387 mL | 0.1936 mL | 0.3872 mL | 0.9680 mL |
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