| Size | Price | Stock | Qty |
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| 5mg |
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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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| Other Sizes |
| Targets |
20(R)-Protopanaxatriol targets peroxisome proliferator-activated receptor gamma (PPARγ), a nuclear receptor that regulates glucose and lipid metabolism, adipocyte differentiation, and inflammation. By acting as a PPARγ antagonist, the compound modulates PPARγ-mediated transcriptional activity, which may have implications for metabolic disorders and cancer. The compound is a natural aglycone of several ginsenosides, which are the bioactive components of ginseng. Its cytotoxicity against leukemia cells suggests additional anticancer mechanisms beyond PPARγ antagonism.
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| ln Vitro |
20(R)-Protopanaxatriol is the ginsenosides Re, Rf, Rg1, Rg2, and Rh's natural aglycone[1].
In vitro, 20(R)-Protopanaxatriol demonstrates cytotoxicity against P388, L1210, and K562 leukemia cells with EC50s of 34, 32, and 38 µM, respectively. As a PPARγ antagonist, it modulates PPARγ-mediated transcriptional activity in cell-based reporter assays. The compound's activity is concentration-dependent, with effective concentrations in the micromolar range. Its natural origin and multi-targeted activity make it a valuable tool for studying ginseng pharmacology, PPARγ signaling, and cancer cell biology. Detailed mechanistic studies are needed to fully characterize its effects on PPARγ and other cellular pathways. |
| ln Vivo |
In vivo, 20(R)-Protopanaxatriol has been studied as a major ginseng constituent with potential therapeutic effects. Its PPARγ antagonist activity may have implications for metabolic disorders such as diabetes and obesity. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources. The compound is primarily used as a research tool for studying ginseng pharmacology, PPARγ signaling, and cancer biology. Further studies are needed to fully characterize its therapeutic potential, dosing regimens, and safety profile in vivo.
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| Enzyme Assay |
The in vitro PPARγ antagonist assay for 20(R)-Protopanaxatriol typically uses cells transfected with a PPARγ expression vector and a luciferase reporter construct containing PPAR-responsive elements. Cells are treated with varying concentrations of the test compound (typically 0.1 to 100 µM) in the presence of a known PPARγ agonist (e.g., rosiglitazone) for 24 hours. Luciferase activity is measured using a luminescence plate reader. The compound's ability to inhibit agonist-induced PPARγ activation is calculated, and IC50 values are determined from dose-response curves using nonlinear regression. For cytotoxicity assays, leukemia cells (P388, L1210, K562) are treated with the compound, and cell viability is assessed using MTT or CellTiter-Glo assays. Positive controls and negative controls are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, leukemia cell lines (P388, L1210, K562) or other cell types are treated with 20(R)-Protopanaxatriol at concentrations ranging from 0.1 to 100 µM for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. PPARγ activity is assessed using luciferase reporter assays or by measuring the expression of PPARγ target genes (e.g., adiponectin, aP2) by qRT-PCR. Apoptosis is quantified by Annexin V/PI staining and caspase activity assays. Cell cycle distribution is analyzed by propidium iodide staining and flow cytometry. All experiments include appropriate controls (vehicle, known PPARγ modulators) and are performed in triplicate.
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| Animal Protocol |
For in vivo studies, 20(R)-Protopanaxatriol may be administered to rodents via oral gavage or intraperitoneal injection at doses ranging from 1 to 50 mg/kg. However, specific in vivo protocols for 20(R)-Protopanaxatriol are not well-documented in publicly available sources. The compound may be used in models of metabolic disorders, cancer, or inflammation. Tissue samples are collected for analysis of PPARγ activity, inflammatory markers, and histological examination. All animal procedures should be conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of 20(R)-Protopanaxatriol have been partially characterized. The compound has a molecular weight of 476.73, a LogP of 5.89, and a tPSA of 69.9. Following oral administration, it shows moderate absorption with a Tmax of 1-3 hours. Plasma half-life is estimated to be 4-8 hours. The compound distributes into tissues including liver, kidney, and adipose tissue. Metabolism is primarily hepatic, with phase II conjugation (glucuronidation, sulfation) as major pathways. The compound is eliminated primarily via biliary and renal excretion. Oral bioavailability is limited due to extensive first-pass metabolism. Further PK studies are needed for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of 20(R)-Protopanaxatriol are limited. As a natural ginseng constituent, it is generally considered to have a favorable safety profile. In acute toxicity studies, the compound is tolerated at moderate doses with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
According to reports, ginseng contains 20(R)-protopanaxadiol, and there is relevant data.
20(R)-Protopanaxatriol (20(R)-APPT) is a natural aglycone of ginsenosides and a novel PPARγ antagonist. It is cytotoxic to leukemia cells (EC50s = 34, 32, 38 µM for P388, L1210, K562). The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent (≥98%) for laboratory use only. Its natural origin and PPARγ antagonist activity make it a valuable tool for studying ginseng pharmacology, PPARγ signaling, metabolic disorders, and cancer biology. |
| Molecular Formula |
C30H52O4
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|---|---|
| Molecular Weight |
476.7315
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| Exact Mass |
476.386
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| CAS # |
1453-93-6
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| PubChem CID |
9847853
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| Appearance |
White to off-white solid
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
590.0±50.0 °C at 760 mmHg
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| Melting Point |
261-263 °C
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| Flash Point |
240.1±24.7 °C
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| Vapour Pressure |
0.0±3.8 mmHg at 25°C
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| Index of Refraction |
1.541
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| LogP |
5.89
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
34
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| Complexity |
817
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| Defined Atom Stereocenter Count |
11
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| SMILES |
O([H])[C@]1([H])C([H])([H])[C@]2([H])[C@@]3(C([H])([H])[H])C([H])([H])C([H])([H])[C@@]([H])(C(C([H])([H])[H])(C([H])([H])[H])[C@]3([H])[C@]([H])(C([H])([H])[C@@]2(C([H])([H])[H])C2(C([H])([H])[H])C([H])([H])C([H])([H])[C@]([H])([C@@](C([H])([H])[H])(C([H])([H])C([H])([H])/C(/[H])=C(\C([H])([H])[H])/C([H])([H])[H])O[H])[C@]21[H])O[H])O[H]
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| InChi Key |
SHCBCKBYTHZQGZ-DLHMIPLTSA-N
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| InChi Code |
InChI=1S/C30H52O4/c1-18(2)10-9-13-30(8,34)19-11-15-28(6)24(19)20(31)16-22-27(5)14-12-23(33)26(3,4)25(27)21(32)17-29(22,28)7/h10,19-25,31-34H,9,11-17H2,1-8H3/t19-,20+,21-,22+,23-,24-,25-,27+,28+,29+,30+/m0/s1
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| Chemical Name |
(3S,5R,6S,8R,9R,10R,12R,13R,14R,17S)-17-[(2R)-2-hydroxy-6-methylhept-5-en-2-yl]-4,4,8,10,14-pentamethyl-2,3,5,6,7,9,11,12,13,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthrene-3,6,12-triol
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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 |
| 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 : ≥ 32 mg/mL (~67.12 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 | 2.0976 mL | 10.4881 mL | 20.9762 mL | |
| 5 mM | 0.4195 mL | 2.0976 mL | 4.1952 mL | |
| 10 mM | 0.2098 mL | 1.0488 mL | 2.0976 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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