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(20S)-Protopanaxadiol P-gp inhibitor

Name: (20S)-Protopanaxadiol
SKU: S4746
Availability: InStock
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Cat.No.S4746

20(S)-Protopanaxadiol (PPD, 20-Epiprotopanaxadiol), the main intestinal metabolite of ginsenosides, is one of the active ingredients in ginseng. 20(S)-Protopanaxadiol inhibits P-glycoprotein in multidrug resistant cancer cells.

Chemical Structure

Molecular Weight: 460.73

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.96%

99.96

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
SF188 cells	Cytotoxicity assay		24 h	Cytotoxicity against human SF188 cells after 24 hrs
U87MG cells	Cytotoxicity assay		24 h	Cytotoxicity against human U87MG cells after 24 hrs
U87MG cells	Function assay		2 h	Increase in superoxide anion level in human U87MG cells after 2 hrs
U87MG cells	Function assay	43.4 μM	4 h	Induction of autophagy in human U87MG cells by MDC staining at 43.4 uM after 4 hrs
U87 cell	Cytotoxicity assay		72 h	Cytotoxicity against human U87 cells after 72 hrs by MTT assay
Hep3B cells	Cytotoxicity assay		72 h	Cytotoxicity against human Hep3B cells after 72 hrs by MTT assay
MDA-MB-231 cells	Function assay	2.5-5.8 μM	24 h	Induction of apoptosis in human MDA-MB-231 cells assessed as increase in expression of cleaved PARP at 2.5 to 5.8 uM after 24 hrs by SDS-polyactylamide gel electrophoresis
LLC-PK1	Cytotoxicity assay		4 h	Cytotoxicity against pig LLC-PK1 cells after 4 hrs by MTT assay
MDA-MB-231 cells	Proliferation assay		4 h	Antiproliferative activity against human MDA-MB-231 cells after 4 hrs by MTT assay
COLO205 cells	Cytotoxicity assay		72 h	Cytotoxicity against human COLO205 cells after 72 hrs by MTT assay
HL60 cells	Cytotoxicity assay		72 h	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
HepG2 cells	Cytotoxicity assay		72 h	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
MCF7 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
SF188 cells	Function assay	108.4 μM	4 h	Induction of autophagy in human SF188 cells by MDC staining at 108.4 uM after 4 hrs
SF188 cells	Function assay	108.4 μM		Activation of caspase 3 in human SF188 cells at 108.4 uM
SF188 cells	Function assay		2 h	Increase in superoxide anion level in human SF188 cells after 2 hrs
SF188 cells	Function assay	108.4 μM		Activation of caspase 7 in human SF188 cells at 108.4 uM
SF188 cells	Function assay	43.4 μM	4 h	Induction of autophagy in human SF188 cells by MDC staining at 43.4 uM after 4 hrs
HepG2 cells	Cytotoxicity assay		48 h	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
HL60 cells	Cytotoxicity assay		48 h	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	460.73	Formula	C₃₀H₅₂O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	30636-90-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	20-Epiprotopanaxadiol			Smiles	CC(=CCCC(C)(C1CCC2(C1C(CC3C2(CCC4C3(CCC(C4(C)C)O)C)C)O)C)O)C

Solubility

In vitro
Batch:

DMSO : 92 mg/mL (199.68 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 33 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

In vitro	Concentrations causing growth inhibition of 50% of cells (LC50) for the compounds PPD is 23 μg/ml, for Int-407 cells. The the LC50 for PPD is determined to be 24 μg/ml in Caco-2 cells. In the Int-407 cell line, PPD produces great percentage of sub-G1 (apoptotic) cells(The Int-407 cell line is a human embryonic nonmalignant cell line originating from fetal tissue of approximately 2 months gestation, whereas Caco-2 is a human colon adenocarcinoma cell line). This response is attributed to differences in individual ginsenoside glycosylation and, thus, the hydrophobic-hydrophilic balance ^[2]. Incubation with PPD also significantly reduces the viability of U251-MG and U87-MG cells in a dose- and time-dependent manner. The cytotoxic effect of PPD is accompanied by reduced expression of cell adhesion proteins, including N-cadherin and integrin β1, which leads to reduced phosphorylation of focal adhesion kinase. Furthermore, incubation with PPD reduces the expression of cyclin D1 and subsequently induces cell-cycle arrest at the G1 phase^[3].
In vivo	Treatment with PPD(20(S)-Protopanaxadiol) and PPT(20(S)-Protopanaxatriol) prior to immobilization stress increase the time spent in open arms and open arm entries in the elevated plus-maze (EPM) test. Treatment with PPD potently suppresses immobilization stress-induced serum levels of corticosterone and interleukin (IL)-6 by the enzyme-linked immunosorbent assay. PPD and PPT may exhibit the anxiolytic effect via γ-aminobutyrateA (GABAA) receptor(s) and serotonergic receptor(s), respectively, and PPD may have an anti-inflammatory effect that is more potent than that of PPT^[1].
References	[1] https://pubmed.ncbi.nlm.nih.gov/25747994/ [2] https://pubmed.ncbi.nlm.nih.gov/15052284/ [3] https://pubmed.ncbi.nlm.nih.gov/26976980/ [4] https://pubmed.ncbi.nlm.nih.gov/19291609/

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