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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Rhapontigenin is a novel and potent analog of resveratrol with multipul bioactivities such as antifungal, anticancer, antioxidant and antibacterial activities. Rhapontigenin is amechanism-based cytochrome P450 1A1 inactivator with IC50 of 400 nM.
ln Vitro |
In HEP G2 cells, rhapontigenin (0-250 μM; 24 hours) demonstrates concentration-dependent anticancer activity with an IC50 of 115 μM [1]. 20 μM; 20 hours) of Rhapontigenin It reduces the amount of TGF-β that triggers certain collagens. TGF-β-induced expression of vimentin, N-cadherin, and CA9 is inhibited in a dependent way by hapontigenin (0 – 20 μM; 6 hours), with IC50 values of 4 and 70 μg/mL, respectively [2–3]. The release of the 13-hexose acidic enzyme brought on by DNP-BSA is inhibited by Rhein. in RBL 2H3 cells, and its IC50 value
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ln Vivo |
Rapontigenin (intraperitoneal injection; 25 mg/kg) has a significant protective effect against death from pulmonary artery thrombosis in mice administered orally 90 minutes before tail vein injection of rapontigenin and collagen [3].
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Cell Assay |
Western Blot analysis [2]
Cell Types: HeLa, A549,769-P Cell Tested Concentrations: 0 μM; 0.03 mM[3]. 2.5μM; 5μM; 10μM; 20 μM Incubation Duration: 6 hrs (hours) Experimental Results: Induces HIF-1α ubiquitination and degradation. |
Animal Protocol |
Animal/Disease Models: ICR mice [3]
Doses: 25mg/kg Administration Doses: 25mg/kg; intraperitoneal (ip) injection Experimental Results:60% anti-thrombotic activity. |
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.
[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. [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. |
Molecular Formula |
C15H14O4
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Molecular Weight |
258.2693
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CAS # |
500-65-2
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O(C([H])([H])[H])C1C([H])=C([H])C(=C([H])C=1O[H])/C(/[H])=C(\[H])/C1C([H])=C(C([H])=C(C=1[H])O[H])O[H]
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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 : ~125 mg/mL (~483.99 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.05 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 20.8 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: ≥ 2.08 mg/mL (8.05 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 20.8 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.8719 mL | 19.3596 mL | 38.7192 mL | |
5 mM | 0.7744 mL | 3.8719 mL | 7.7438 mL | |
10 mM | 0.3872 mL | 1.9360 mL | 3.8719 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.