1. Immunology/Inflammation Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Apoptosis
  2. Glucocorticoid Receptor Estrogen Receptor/ERR LXR Apoptosis
  3. (20S)-Protopanaxatriol

(20S)-Protopanaxatriol  (Synonyms: 20(S)-APPT; g-PPT)

Cat. No.: HY-N0835 Purity: 99.42%
COA Handling Instructions

(20S)-Protopanaxatriol is a metabolite of ginsenoside. (20S)-Protopanaxatriol works through the glucocorticoid receptor (GR) and estrogen receptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects.

For research use only. We do not sell to patients.

(20S)-Protopanaxatriol Chemical Structure

(20S)-Protopanaxatriol Chemical Structure

CAS No. : 34080-08-5

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10 mM * 1 mL in DMSO
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Description

(20S)-Protopanaxatriol is a metabolite of ginsenoside. (20S)-Protopanaxatriol works through the glucocorticoid receptor (GR) and estrogen receptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects[1][2][3].

IC50 & Target

Glucocorticoid receptor, Oestrogen receptor[1];
LXRα[2]

In Vitro

(20S)-Protopanaxatriol works through the glucocorticoid receptor (GR) and oestrogen receptor (ER) in human umbilical vein endothelial cells (HUVECs). (20S)-Protopanaxatriol (PPT) increases [Ca2+]i with an EC50 of 482 nM in HUVECs. ((20S)-Protopanaxatriol (1 µM) elevates NO production via ERβ[1]. (20S)-Protopanaxatriol inhibits the autonomous transactivation of Gal4-LXRα LBD, the T0901317-dependent transcription of SREBP-1c and its promoter. (20S)-Protopanaxatriol (10 μg/mL) blocks the recruitment of RNA polymerase II to the LXRE region of SREBP-1c. (20S)-Protopanaxatriol also inhibits T0901317-dependent transcription of LXRα target genes related to lipogenesis, and reduces T0901317-induced cellular triglyceride (TG) accumulation in primary hepatocytes, but does not alter transcription of ABCA1, also an LXRα target gene[2].
Both In HCC827GR and H1975 cell lines, g-PPT (100 nM, 1 μM, 10 μM, 20 μM; 48 hours) results in SCD1 expression decreased[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

(20S)-Protopanaxatriol (10 mg/kg; i.p.; daily for four weeks) synergizes with Gefitinib to inhibit xenograft growth[3].
(20S)-Protopanaxatriol (50-100 mg/kg; p.o.; 25 days; female BALB/c nude mice bearing breast cancer MCF-7 cell) inhibits the growth of MCF-7 breast cancer cells in a nude mice xenograft assay[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: H1975 murine xenograft tumor model
Dosage: 10 mg/kg
Administration: I.p.; daily for four weeks
Result: The combined g-PPT and Gefitinib (50 mg/kg/day) treatment clearly reduced p-EGFR and KI67 expression and increased c-Caspase3 expression compared to Gefitinib or g-PPT treatment alone.
Molecular Weight

476.73

Formula

C30H52O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@]([C@@](C[C@H]1O)([H])[C@]2(CC[C@@H]3O)C)(C[C@H](O)[C@@]2([H])C3(C)C)[C@]4([C@@]1([H])[C@]([C@@](C)(O)CC/C=C(C)/C)([H])CC4)C

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (209.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.36 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.36 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.42%

References

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. 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 2.0976 mL 10.4881 mL 20.9762 mL 52.4406 mL
5 mM 0.4195 mL 2.0976 mL 4.1952 mL 10.4881 mL
10 mM 0.2098 mL 1.0488 mL 2.0976 mL 5.2441 mL
15 mM 0.1398 mL 0.6992 mL 1.3984 mL 3.4960 mL
20 mM 0.1049 mL 0.5244 mL 1.0488 mL 2.6220 mL
25 mM 0.0839 mL 0.4195 mL 0.8390 mL 2.0976 mL
30 mM 0.0699 mL 0.3496 mL 0.6992 mL 1.7480 mL
40 mM 0.0524 mL 0.2622 mL 0.5244 mL 1.3110 mL
50 mM 0.0420 mL 0.2098 mL 0.4195 mL 1.0488 mL
60 mM 0.0350 mL 0.1748 mL 0.3496 mL 0.8740 mL
80 mM 0.0262 mL 0.1311 mL 0.2622 mL 0.6555 mL
100 mM 0.0210 mL 0.1049 mL 0.2098 mL 0.5244 mL
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(20S)-Protopanaxatriol
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