GLPBio

Tocofersolan

Catalog No.: GC31315Purity:>95.00%Synonyms: Tocophersolan, D-α-Tocopheryl Polyethylene Glycol Succinate, TPGS 1000, VE-TPGS, Vitamin E TPGS
COASDSData Sheet

Tocofersolan is a polyethylene glycol derivative of α-tocopherol and is a water-soluble vitamin E analog.

Products are for research use only. Not for human use. We do not sell to patients.

Tocofersolan
Cas No.: 9002-96-4
10mM (in 1mL DMSO)In Stock
$40.00
1
500mgIn Stock
$32.00
1
5gIn Stock
$40.00
1
10gIn Stock
$64.00
1
25gIn Stock
$128.00
1
50gIn Stock
$198.00
1
100gIn Stock
$298.00
1
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Description

Tocofersolan is a polyethylene glycol derivative of α-tocopherol and is a water-soluble vitamin E analog[1]. Tocofersolan has antioxidant activity and serves as an orally bioavailable source of vitamin E[2]. Tocofersolan increases the solubility and bioavailability of some drugs, and improves their pharmacokinetic properties[3]. Tocofersolan is usually used in drug delivery systems or nutraceuticals[4][5].

In vitro, Tocofersolan (3.3µM to 16.5mM; 60min) inhibited P-glycoprotein (P-gp) - mediated drug efflux in Caco-2 cells with an IC50 of 5.86µM[6].

In vivo, Tocofersolan (1µM) co-exposure for 5 days post-fertilization in larval zebrafish reversed the locomotor hypoactivity caused by benzo[a]pyrene (5µM) exposure[7].

References:
[1] Sadoqi M, Lau-Cam CA, Wu SH. Investigation of the micellar properties of the tocopheryl polyethylene glycol succinate surfactants TPGS 400 and TPGS 1000 by steady state fluorometry. J Colloid Interface Sci. 2009;333(2):585-589.
[2] Thebaut A, Nemeth A, Le Mouhaer J, et al. Oral Tocofersolan Corrects or Prevents Vitamin E Deficiency in Children With Chronic Cholestasis. J Pediatr Gastroenterol Nutr. 2016;63(6):610-615.
[3] Wande DP, Cui Q, Chen S, Xu C, Xiong H, Yao J. Rediscovering Tocophersolan: A Renaissance for Nano-Based Drug Delivery and Nanotheranostic Applications. Curr Drug Targets. 2021;22(8):856-869.
[4] Tan S, Zou C, Zhang W, Yin M, Gao X, Tang Q. Recent developments in d-α-tocopheryl polyethylene glycol-succinate-based nanomedicine for cancer therapy. Drug Deliv. 2017;24(1):1831-1842.
[5] Srivastava A, Lall R, Talukder J, DuBourdieu D, Gupta RC. Iron Transport Tocopheryl Polyethylene Glycol Succinate in Animal Health and Diseases. Molecules. 2019;24(23):4289.
[6] Collnot EM, Baldes C, Wempe MF, et al. Mechanism of inhibition of P-glycoprotein mediated efflux by vitamin E TPGS: influence on ATPase activity and membrane fluidity. Mol Pharm. 2007;4(3):465-474.
[7] Holloway Z, Hawkey A, Asrat H, Boinapally N, Levin ED. The use of tocofersolan as a rescue agent in larval zebrafish exposed to benzo[a]pyrene in early development. Neurotoxicology. 2021;86:78-84.

Protocol

Cell experiment [1]:

Cell lines

 Caco-2 cells

Preparation Method

 Caco-2 cells were grown to 90% confluence in 75cm2 T-flasks with DMEM supplemented with 10% FBS and 1% NEAA. Culture media were changed every second day, and cells were grown at a temperature of 37°C in an atmosphere of 85% relative humidity and 5% CO2. Trypsinized Caco-2 cells were spin labeled by incubating a suspension (2.0×107 cells/mL) in Krebs Ringer Buffer (KRB; pH 7.4) for 30min at 37°C with 0.5mM of a spin label stock solution (10mM 5-doxyl stearic acid (5-SA) in ethanol). Different concentrations of Tocofersolan (3.3µM to 16.5mM) were added via stock solutions, and cell suspensions were incubated for 60min. After suspension centrifugation (4min at 1200g), supernatant was removed and the cell pellet was washed and resuspended in KRB to give a final concentration of 1.0×108 cells/mL. To quench residual free spin label, chrome oxalate (final concentration 2.0mM) was added and the ensuing cell suspension (100µL) was filled into the test tube and placed in a 4103 TM/ 8609 cavity. ESR measurements were performed at room temperature using a Bruker ESP300 E spectrometer with an ER081 (90/30 C5) magnet. Cell membrane fluidity was depicted via the cell membrane order parameter S. S can be derived from the ESR spectral line splitting.

Reaction Conditions

 3.3µM to 16.5mM; 60min

Applications

 Tocofersolan had negligible effects on Caco-2 cell membrane fluidity at concentrations up to 0.33mM, but significant fluidization effects were observed at higher concentrations (above 1.65mM).

References:
[1] Collnot EM, Baldes C, Wempe MF, et al. Mechanism of inhibition of P-glycoprotein mediated efflux by vitamin E TPGS: influence on ATPase activity and membrane fluidity. Mol Pharm. 2007;4(3):465-474.

Product Documents

Purity:>95.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
9002-96-4
Synonyms
Tocophersolan, D-α-Tocopheryl Polyethylene Glycol Succinate, TPGS 1000, VE-TPGS, Vitamin E TPGS
SMILES
CC1=C(CCC(CCCC(C)CCCC(C)CCCC(C)C)(C)O2)C2=C(C)C(C)=C1OC(CCC(OCCO)=O)=O.[n]
Molecular Formula
C35H58O6
Molecular Weight
1513.00
Solubility
DMSO : 31.25 mg/mL (20.65 mM);Water : < 0.1 mg/mL (insoluble)
Storage
Store at -20°C,protect from light
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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