| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
| ln Vitro |
(20S)-Protopanaxatriol acts on human umbilical vein endothelial cells (HUVEC) via the glucocorticoid receptor (GR) and estrogen receptor (ER). With an EC50 of 482 nM, (20S)-Protopanaxatriol (PPT) raises [Ca2+]i in HUVEC. NO production is increased by ((20S)-Protopanaxatriol at 1 µM via ERβ [1]. (20S)-Protopanaxatriol inhibits SREBP-1c and its promoter's autonomous transactivation of Gal4-LXRα LBD. transcription dependent on T0901317. (20S)-Protopanaxatriol (10 μg/mL) inhibits RNA polymerase II's recruitment to the SREBP-1c LXRE region. Additionally, T0901317-dependent transcription of LXRα target genes involved in adipogenesis is inhibited by (20S)-Protopanaxatriol. LXRα target gene ABCA1's transcription was unaffected by transcription, although T0901317-induced cellular triglyceride (TG) accumulation in primary hepatocytes was decreased [2]. g-PPT (100 nM, 1 μM, 10 μM, 20 μM; 48 hours) decreased the expression of SCD1 in HCC827GR and H1975 cell lines [3].
|
|---|---|
| ln Vivo |
(20S)-Protopanaxatriol (10 mg/kg; intraperitoneally; once daily for four weeks) and Gefitinib work together to suppress xenograft growth [3]. (20S)-Protopanaxatriol suppresses the development of MCF-7 breast cancer cells in a nude mouse xenograft experiment (50–100 mg/kg; oral; 25 days; female BALB/c nude mice harboring breast cancer MCF-7 cells) [4].
|
| Animal Protocol |
Animal/Disease Models: H1975 mouse xenograft tumor model
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection; Experimental Results: Compared with gefitinib or g-PPT treatment alone, g-PPT and gefitinib (50 mg/kg kg/day) combined treatment Dramatically diminished p-EGFR and KI67 expression and increased c-Caspase3 expression. |
| References |
[1]. 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.
[2]. 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. [3]. 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. [4]. Zhang H, et al. 20(S)-Protopanaxadiol-Induced Apoptosis in MCF-7 Breast Cancer Cell Line through the Inhibition of PI3K/AKT/mTOR Signaling Pathway. Int J Mol Sci. 2018;19(4):1053. Published 2018 Apr 2. |
| Molecular Formula |
C30H52O4
|
|---|---|
| Molecular Weight |
476.7315
|
| CAS # |
34080-08-5
|
| 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])[C@]2(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]
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~209.76 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.36 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 (4.36 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.36 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
