| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 5g |
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| Other Sizes |
| ln Vitro |
In Caco-2 intestinal epithelial cells, Glycodeoxycholate Sodium exhibited an IC50 of 2.0 mM in the MTS cytotoxicity assay after 120 min exposure. It reduced transepithelial electrical resistance (TEER) and increased the apparent permeability coefficient (Papp) of [¹⁴C]-mannitol across Caco-2 monolayers at 0.5 mM. At 10 mM, it increased the Papp of FITC-dextran 4000 (FD4) and FITC-LKP across isolated rat colonic mucosae. In the buccal epithelial cell line TR146, the IC50 was 1.9 mM in the MTS assay. It also increased the Papp of FD4 across TR146 multilayers at 1.5 mM and induced actin rearrangement. High-content analysis (HCA) in Caco-2 and TR146 cells showed that GDC altered nuclear area, nuclear intensity, mitochondrial membrane potential, and plasma membrane potential at concentrations ≥1.5 mM. [1]
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| Cell Assay |
Cytotoxicity Assays: Caco-2 and TR146 cells were seeded in 96-well plates and exposed to GDC for 120 min. Viability was assessed using MTS, CellTox Green (membrane integrity), Caspase-Glo 3/7 (apoptosis), ROS-Glo H₂O₂ (reactive oxygen species), JC-1 (mitochondrial membrane potential), Laurdan (membrane fluidity), and RealTime-Glo Annexin V (apoptosis/necrosis) assays. High-content analysis (HCA) was performed using dyes for nuclei (Hoechst 33342), intracellular calcium (Fluo-4 AM), mitochondria (TMRM), and dead cells (TOTO-3 iodide). [1]
Permeability Assay: Caco-2 monolayers or TR146 multilayers grown on Transwell filters were used. TEER was measured before and after apical addition of GDC. The Papp of markers ([¹⁴C]-mannitol, FD4, FITC-LKP, [³H]-octreotide) was calculated from basolateral samples collected over 120 min. [1] Immunocytochemistry: TR146 cells grown on chamber slides were exposed to GDC, fixed, permeabilized, stained with Alexa Fluor 488 Phalloidin (F-actin) and Hoechst (nuclei), and imaged by confocal microscopy. [1] |
| Animal Protocol |
Rat Colonic Mucosae: Male Wistar rats (250–300 g) were euthanized, and colonic tissue was dissected. The smooth muscle layer was removed, and mucosae were mounted in Ussing chambers. Tissues were bathed in Krebs-Henseleit buffer at 37°C. GDC was added apically, and TEER and Papp of markers were monitored over 120 min. [1]
Porcine Buccal Mucosae: Buccal tissue from pigs was collected post-mortem, trimmed, and the epithelial layer was prepared using a dermatome. Tissues were mounted in Ussing chambers, equilibrated, and treated apically with GDC. TEER and Papp of markers were measured over 3 h. [1] |
| Toxicity/Toxicokinetics |
In Caco-2 cells, GDC showed low cytotoxicity at concentrations ≤2 mM. In isolated rat colonic mucosa, 10 mM GDC did not cause any histologically visible damage. In porcine buccal mucosa, GDC at concentrations up to 10 mM did not induce histological changes. At concentrations >0.5 mM, GDC primarily induced necrosis rather than apoptosis in TR146 cells. [1]
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| References |
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| Additional Infomation |
Glucose deoxycholic acid is a glycine conjugate of deoxycholic acid, a human metabolite that is functionally related to deoxycholic acid and is also a conjugated acid of glycodeoxycholic acid salt. Glucose deoxycholic acid has been reported in Streptomyces nigricans, Trypanosoma brevicornu, and Caenorhabditis elegans, and there is relevant data. Glucose deoxycholic acid is a bile salt formed by the conjugation of deoxycholic acid with glycine in the liver, and is usually present in the form of sodium salt. It is a surfactant that can dissolve fats to promote absorption and is also absorbed itself. It is used as a choleretic agent and choleretic drug. Sodium glycodeoxycholate is a secondary bile salt with amphiphilic surfactant properties. It promotes permeation by increasing cell membrane fluidity, temporarily opening tight junctions, and altering the tissue structure of the actin cytoskeleton. It is being explored for oral and buccal delivery of macromolecules such as peptides and is one of the components of some oral peptide formulations in clinical stages. Its critical micelle concentration (CMC) ranges from 2 to 6 mM. [1]
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| Molecular Formula |
C26H42NNAO5
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|---|---|
| Molecular Weight |
471.6052
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| Exact Mass |
449.314
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| CAS # |
16409-34-0
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| Related CAS # |
Glycodeoxycholic Acid;360-65-6;Glycodeoxycholic acid monohydrate;1079043-81-4
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| PubChem CID |
3035026
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| Appearance |
White to off-white solid powder
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| Density |
0.9330g/cm3
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| Boiling Point |
655.6ºC at 760 mmHg
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| Melting Point |
207 °C
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| Flash Point |
350.3ºC
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| Vapour Pressure |
5.74E-20mmHg at 25°C
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| LogP |
2.65
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
32
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| Complexity |
727
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| Defined Atom Stereocenter Count |
10
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| SMILES |
C[C@H](CCC(=O)NCC(=O)O)[C@H]1CC[C@@H]2[C@@]1([C@H](C[C@H]3[C@H]2CC[C@H]4[C@@]3(CC[C@H](C4)O)C)O)C
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| InChi Key |
WVULKSPCQVQLCU-BUXLTGKBSA-N
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| InChi Code |
InChI=1S/C26H43NO5/c1-15(4-9-23(30)27-14-24(31)32)19-7-8-20-18-6-5-16-12-17(28)10-11-25(16,2)21(18)13-22(29)26(19,20)3/h15-22,28-29H,4-14H2,1-3H3,(H,27,30)(H,31,32)/t15-,16-,17-,18+,19-,20+,21+,22+,25+,26-/m1/s1
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| Chemical Name |
2-[[(4R)-4-[(3R,5R,8R,9S,10S,12S,13R,14S,17R)-3,12-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]acetic acid
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ≥ 150 mg/mL (~318.06 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.30 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 25.0 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: ≥ 2.5 mg/mL (5.30 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 25.0 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: ≥ 2.5 mg/mL (5.30 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 | 2.1204 mL | 10.6020 mL | 21.2040 mL | |
| 5 mM | 0.4241 mL | 2.1204 mL | 4.2408 mL | |
| 10 mM | 0.2120 mL | 1.0602 mL | 2.1204 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.
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