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Cholic acid

Catalog No.GN10623

Cholic acid Chemical Structure

A primary bile acid

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10mM (in 1mL DMSO)
$34.00
In stock
20mg
$20.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

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Protocol

Cell experiment:

HepG2 cells are pretreated with the inhibitors NaN3 (1 mg/mL), Genistein (50 μg/mL), MβCD (10 mM), Nystatin (50 μg/mL), Chlorpromazine (10 μg/mL), and Cholic acid (1 mg/mL) for 30 min. After removing the inhibitors, the cells are incubated with CA-LPs for 2 h, and the cellular uptake of LPs is determined in the "In vitro cellular uptake assays" section[1].

Animal experiment:

Mice[2] Tg-CYP2D6 mice are fed with normal chow (control) or 1% (w/w) Cholic acid-supplemented diet (CA) for 14 days (n=4 mice/group). Alkaline phosphatase (ALP) and alanine aminotransferase (ALT) activities are measured in mouse serum.

References:

[1]. Li Y, et al. Mechanism of hepatic targeting via oral administration of DSPE-PEG-Cholic acid-modified nanoliposomes. Int J Nanomedicine. 2017 Feb 28;12:1673-1684.
[2]. Pan X, et al. Cholic acid Feeding Leads to Increased CYP2D6 Expression in CYP2D6-Humanized Mice. Drug Metab Dispos. 2017 Apr;45(4):346-352.

Background

Cholic acid is a major primary bile acid produced in the liver and usually conjugated with glycine or taurine. It facilitates fat absorption and cholesterol excretion.

Cholic acid competitively binds Na+/taurocholate cotransporting polypeptide (NTCP) on HepG2 cells and significantly inhibits the uptake of Cholic acid (CA)-nanoliposomes (LPs)-Doxorubicin (DOX)-HCl, which indicates that CA-LPs-DOX-HCl are also uptaken via NTCP-mediated endocytosis pathway[1].

Cholic acid feeding leads to increased CYP2D6 expression in CYP2D6-humanized mice. As a cholestasis model, Tg-CYP2D6 mice are fed a Cholic acid (CA)-supplemented diet for over 1 week. The treatment is known to increase bile acid pool size by 2-fold and to replace ~90% of bile acids with CA, recapitulating the features of cholestatic conditions in humans[2].

References:
[1]. Li Y, et al. Mechanism of hepatic targeting via oral administration of DSPE-PEG-Cholic acid-modified nanoliposomes. Int J Nanomedicine. 2017 Feb 28;12:1673-1684.
[2]. Pan X, et al. Cholic acid Feeding Leads to Increased CYP2D6 Expression in CYP2D6-Humanized Mice. Drug Metab Dispos. 2017 Apr;45(4):346-352.

Chemical Properties

Cas No. 81-25-4 SDF
Chemical Name (4R)-4-[(3R,5S,7R,8R,9S,10S,12S,13R,14S,17R)-3,7,12-trihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid
Canonical SMILES CC(CCC(=O)O)C1CCC2C1(C(CC3C2C(CC4C3(CCC(C4)O)C)O)O)C
Formula C24H40O5 M.Wt 408.58
Solubility ≥ 20.5mg/mL in Ethanol Storage
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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

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