(20S)-Protopanaxatriol (g-PPT, 20(S)-APPT), a neuroprotective metabolite of ginsenoside, protopanaxatriol (g-PPT), is a functional ligand for both GR and ERbeta and could modulate endothelial cell functions through the glucocorticoid receptor (GR) and estrogen receptor (ER).
CAS Number: 34080-08-5
Molecular Weight: 476.73
Chemical Name: (1S,3aR,3bR,5S,5aR,7S,9aR,9bR,11R,11aR)-1-[(2S)-2-hydroxy-6-methylhept-5-en-2-yl]-3a,3b,6,6,9a-pentamethyl-hexadecahydro-1H-cyclopenta[a]phenanthrene-5,7,11-triol
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (209.76 mM; Need ultrasonic)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
(20S)-Protopanaxatriol works through the glucocorticoid receptor (GR) and oestrogen receptor (ER) in human umbilical vein endothelial cells (HUVECs). (20S)-Protopanaxatriol (g-PPT) increases [Ca2+]i with an EC50 of 482 nM in HUVECs. (20S)-Protopanaxatriol (1 µM) elevates NO production via ERβ. (20S)-Protopanaxatriol (PPT) 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. Both In HCC827GR and H1975 cell lines, g-PPT (100 nM, 1 μM, 10 μM, 20 μM; 48 hours) results in SCD1 expression decreased.
(20S)-Protopanaxatriol (10 mg/kg; i.p.; daily for four weeks) synergizes with Gefitinib to inhibit xenograft growth. 20(S)-PPD (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.
- Leung KW, et al. Protopanaxadiol and protopanaxatriol bind to glucocorticoid and oestrogen receptors in endothelial cells. Br J Pharmacol. 2009 Feb;156(4):626-37.
- Oh GS, et al. 20(S)-protopanaxatriol inhibits liver X receptor α-mediated expression of lipogenic genes in hepatocytes. J Pharmacol Sci. 2015 Jun;128(2):71-7.
- Huang Q, et al. Co-administration of 20(S)-protopanaxatriol (g-PPT) and EGFR-TKI overcomes EGFR-TKI resistance by decreasing SCD1 induced lipid accumulation in non-small cell lung cancer. J Exp Clin Cancer Res. 2019;38(1):129. Published 2019 Mar 15.
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