Taurolithocholic acid

Name: Taurolithocholic acid
Brand: MedChemExpress
SKU: HY-113308
Rating: 5.0 (6 reviews)

Cat. No.: HY-113308 Purity: 98.38%: Data Sheet
COA

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Taurolithocholic acid is an orally active bile acid and antiviral agent. Taurolithocholic acid upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis (Ferroptosis), viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic acid also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic acid serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic acid shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic acid not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis.

For research use only. We do not sell to patients.

CAS No. : 516-90-5

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Taurolithocholic acid:

Taurolithocholic acid-d₄ sodium In-stock
Taurolithocholic acid-d₄ In-stock
Taurolithocholic acid sodium salt In-stock
Taurolithocholic acid-d₅ Get quote

6 Publications Citing Use of MCE Taurolithocholic acid

RT-PCR

: Taurolithocholic acid purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Feb 3:e2411719. [Abstract]; The mRNA levels of ALDOB in Huh7 or HCCLM3 cells treated with various bile acids (100 μM, 24 h). All data are presented as mean ± SD. Data were analyzed by one-way ANOVA with Bonferroni multiple-comparison correction. CA, cholic acid; TCA, taurocholic acid; GCA, glycocholic acid; TCDCA, taurochenodeoxycholic acid; GCDCA, glycochenodeoxycholic acid; LCA, lithocholic acid; TLCA, taurolithocholic acid; GLCA, glycolithocholic acid; DCA, deoxycholic acid; TDCA, taurodeoxycholic acid; GDCA, glycodeoxycholic acid; UDCA, ursodeoxycholic acid; TUDCA, tauroursodeoxycholic acid; GUDCA, glycoursodeoxycholic acid.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Human Endogenous Metabolite

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.29 μM Compound: 6a, tauro	Agonist activity at human TGR5 expressed in CHO cells by luciferase assay Agonist activity at human TGR5 expressed in CHO cells by luciferase assay	[PMID: 18307294]
CHO	EC₅₀	0.847 μM Compound: TLCA	Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay	[PMID: 31268316]
CHO	EC₅₀	330 nM Compound: TLCA	Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation in presence of 3-isobutyl-1-methylxanthine after 20 mins Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation in presence of 3-isobutyl-1-methylxanthine after 20 mins	[PMID: 31268316]
HEK-293T	EC₅₀	> 150 μM Compound: TLCA	Agonist activity at VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay Agonist activity at VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay	[PMID: 26774929]
HEK-293T	IC₅₀	> 50 μM Compound: TLCA	Antagonist activity against VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as inhibition of 1,25-dihydroxyvitamin D3-induced SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay Antagonist activity against VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as inhibition of 1,25-dihydroxyvitamin D3-induced SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay	[PMID: 26774929]
HEK293	IC₅₀	20 μM Compound: Taurolithocholate	TP_TRANSPORTER: inhibition of E217betaG uptake in membrane vesicles from MRP4-expressing HEK-293 cells TP_TRANSPORTER: inhibition of E217betaG uptake in membrane vesicles from MRP4-expressing HEK-293 cells	[PMID: 12523936]

In Vitro

Taurolithocholic acid (50-200 μM; 24 h) dose-dependently inhibits SFTSV replication in human THP-1 monocytic cells without inducing cytotoxicity^[1].
Taurolithocholic acid (50-200 μM; 24 h) dose-dependently inhibits HRTV replication in human THP-1 monocytic cells^[1].
Taurolithocholic acid (16 h) inhibits the post-entry replication stage of SFTSV infection in human THP-1 monocytic cells, reducing intracellular viral RNA levels and infection rate by approximately 50% when added post-infection or throughout the 16 h infection period^[1].
Taurolithocholic acid (50-200 μM) dose-dependently inhibits SFTSV mini-genome activity in BSR-T7 cells^[1].
Taurolithocholic acid (50-200 μM; 24 h) dose-dependently suppresses SFTSV-induced IL-1β production and NF-κB activation in human THP-1 monocytic cells^[1].
Taurolithocholic acid (200 μM; 24 h) upregulates FADS2 expression in SFTSV-infected human THP-1 monocytic cells, reversing SFTSV-induced FADS2 downregulation^[1].
Taurolithocholic acid (0-24 h) time-dependently activates the TGR5-PI3K/AKT-SREBP2 pathway and upregulates FADS2 in human THP-1 monocytic cells over 0 to 24 h^[1].
Taurolithocholic acid (100 μM; 24 h) alleviates SFTSV-induced ferroptosis in murine BMDMs, as measured by reduced lipid ROS and LDH release^[1].
Taurolithocholic acid (100 μM; pre-treatment, followed by 24 h incubation with ferroptosis agonists) inhibits Fe²⁺- and RSL-3-induced ferroptosis in murine BMDMs via upregulation of FADS2, as shown by reduced lipid ROS and LDH release which is reversed by FADS2 inhibition^[1].
Taurolithocholic acid (5 μM; 4 h) induces robust apoptosis in Ntcp-transfected HepG2 cells, increasing the percentage of apoptotic cells to 65.5% of total cells^[2].
Taurolithocholic acid (2.5-5 μmol/liter; 20 min total incubation) impairs canalicular bile acid secretion by 54% and 60%, respectively, without affecting substrate uptake in isolated rat hepatocyte couplets^[3].
Taurolithocholic acid (5 μmol/liter; 5-60 min) induces sustained activation of PKB/Akt, increasing activity to 194% of control levels after 60 min in isolated rat hepatocytes^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[2]

Cell Line:	Ntcp-transfected human hepatoma (HepG2) cells
Concentration:	5 μM
Incubation Time:	4 h
Result:	Increased the rate of apoptotic cell death to 65.5 ± 34.1% of total cells, compared to 1.5 ± 1.0% in control cells.

In Vivo

Taurolithocholic acid (final concentration in cerebrospinal fluid: 1 μM; chronic intracerebroventricular infusion; continuous constant-rate administration; 8-day treatment period) significantly increases the global fat oxidation rate, reduces body fat content by 26%, induces browning of subcutaneous white adipose tissue and decreases adipocyte volume, without affecting total body weight, food intake, spontaneous activity or plasma bile acid levels in male C57Bl/6J mice fed a regular chow diet^[4].
Taurolithocholic acid (final concentration of 1 μM in cerebrospinal fluid; chronic intracerebroventricular infusion; continuous constant-rate administration; treatment duration of 23 days) significantly enhances the uptake of triglyceride-derived fatty acids by brown adipose tissue, upregulates the mRNA expression of thermogenesis-related genes such as Lpl, Tgr5, Dio2 and Ucp1 in brown adipose tissue, and exerts no effect on energy expenditure, body weight or gonadal white adipose tissue weight in male C57Bl/6J mice fed a high-fat diet^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male C57Bl/6J mice (male, 15 weeks old), fed with high fat diet (HFD, energetic content: 45% fat, 35% carbohydrates, 20% protein)^[4]
Dosage:	Final concentration of 1 μM in cerebrospinal fluid,
Administration:	chronic intracerebroventricular (i.c.v.) infusion
Result:	Significantly enhanced the uptake of triglyceride-derived fatty acids from [³H]TO-labeled emulsion particles by subscapular brown adipose tissue (sBAT), and markedly upregulated the mRNA expression of thermogenic genes including Lpl, Tgr5, Dio2 and Ucp1 in interscapular brown adipose tissue (iBAT). It showed a trend of increased Ucp1 mRNA expression in subcutaneous white adipose tissue (sWAT), and had no effect on energy expenditure, body weight, gonadal white adipose tissue (gWAT) weight, and the uptake of triglyceride-derived fatty acids by white adipose tissue depots.

Molecular Weight

483.70

Formula

C₂₆H₄₅NO₅S

CAS No.

516-90-5

Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12[C@](CC[C@]2([H])[C@H](C)CCC(NCCS(=O)(O)=O)=O)([H])[C@@]3([H])[C@@](CC1)([H])[C@@]4([C@](C[C@@H](CC4)O)([H])CC3)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 16.67 mg/mL (34.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0674 mL	10.3370 mL	20.6740 mL
5 mM	0.4135 mL	2.0674 mL	4.1348 mL
10 mM	0.2067 mL	1.0337 mL	2.0674 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (3.45 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.67 mg/mL (3.45 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.67 mg/mL (3.45 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.7%

Select Batch:

Data Sheet (281 KB) SDS (419 KB)

COA (247 KB)

Handling Instructions (2659 KB)

References

[1]. Zheng X, et al. Taurolithocholic acid protects against viral haemorrhagic fever via inhibition of ferroptosis. Nat Microbiol. 2024;9(10):2583-2599. [Content Brief]

[2]. Denk GU, et al. Conjugation is essential for the anticholestatic effect of NorUrsodeoxycholic acid in taurolithocholic acid-induced cholestasis in rat liver. Hepatology. 2010;52(5):1758-1768. [Content Brief]

[3]. Beuers U, et al. Taurolithocholic acid exerts cholestatic effects via phosphatidylinositol 3-kinase-dependent mechanisms in perfused rat livers and rat hepatocyte couplets. J Biol Chem. 2003;278(20):17810-17818. [Content Brief]

[4]. Eggink H M, Tambyrajah L L, van den Berg R, et al. Chronic infusion of taurolithocholate into the brain increases fat oxidation in mice[J]. Journal of Endocrinology, 2018, 236(2): 85-97.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0674 mL	10.3370 mL	20.6740 mL	51.6849 mL
	5 mM	0.4135 mL	2.0674 mL	4.1348 mL	10.3370 mL
	10 mM	0.2067 mL	1.0337 mL	2.0674 mL	5.1685 mL
	15 mM	0.1378 mL	0.6891 mL	1.3783 mL	3.4457 mL
	20 mM	0.1034 mL	0.5168 mL	1.0337 mL	2.5842 mL
	25 mM	0.0827 mL	0.4135 mL	0.8270 mL	2.0674 mL
	30 mM	0.0689 mL	0.3446 mL	0.6891 mL	1.7228 mL