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Lithocholic acid

Name: Lithocholic acid
Brand: TargetMol
SKU: T2202
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2202Cas No. 434-13-9

Alias 3α-Hydroxy-5β-cholanic acid

Lithocholic acid (3α-Hydroxy-5β-cholanic acid) is a toxic secondary bile acid, They were FXR antagonists (IC50=0.7, 1.4 μM), EphA2 antagonists (IC50=48, 66 μM) and EphB4 antagonists (IC50=141 μM). Lithocholic acid can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is a cleanser that dissolves fat for absorption and is itself absorbed.

Lithocholic acid

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Purity: 99.93%

Catalog No. T2202Alias 3α-Hydroxy-5β-cholanic acidCas No. 434-13-9

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
500 mg	$29	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$29	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.93%

Color:White

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Product Introduction

Bioactivity

Description	Lithocholic acid (3α-Hydroxy-5β-cholanic acid) is a toxic secondary bile acid, They were FXR antagonists (IC50=0.7, 1.4 μM), EphA2 antagonists (IC50=48, 66 μM) and EphB4 antagonists (IC50=141 μM). Lithocholic acid can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is a cleanser that dissolves fat for absorption and is itself absorbed.
Targets&IC50	USP2a:31.1 ± 3.4 µM, PC3 cells:32.0 µM, HCT116 cells (wt):46.8 ± 2.6 μM (LD50), DU-145 cells:30.4 µM, HCT116 cells (p53−/−):37.4 ± 3.8 μM (LD50)
In vitro	METHODS: Human A549, HCT-116, HT-29, Huh-7, LoVo, MGC-803, RKO, SK-HEP1, SW480 cells were treated with Lithocholic acid (200, 100, 50, P < 0.05). 25, 12.5, 6.25, 3.125, 1.5625 μM) were used to detect the cell growth inhibition by MTT method. RESULTS: Lithocholic acid did not affect the growth of A549, HCT-116, HT-29, Huh-7, LoVo, MGC-803, RKO, SK-HEP1, and SW480 cells (IC50> 200 µM). [1] METHODS: Human Caco2 and HT-1080 cells were treated with Lithocholic acid (0.1-1000 μM) for 24 hours, and the cytotoxicity was detected by MTT assay. RESULTS: Lithocholic acid significantly inhibited the growth of Caco2 (IC50=56 μM) and HT-1080 cells (IC50=23 μM). [2] METHODS: Human DLD1, HCT-116, and HCT-8 cells were treated with Lithocholic acid (25, 50, 100, 150, and 200μM) for 48 hours, and the cytotoxicity was detected by MTT assay. RESULTS: Lithocholic acid significantly inhibited the growth of human DLD1 (IC50=173.1 μM), HCT-116 (IC50=81.1 μM) and HCT-8 (IC50=97.4 μM) cells. [3]
In vivo	METHODS: To investigate the antiviral effect of Lithocholic acid, Lithocholic acid oleate (3%) and Lithocholic acid (0.5%), derivatives of LCA, were administered to HSV-1 virus infected mice. RESULTS: Mice treated with Lithocholic acid oleate+Lithocholic acid 48 hours before virus inoculation showed lesions on day 6 after infection, and the wound healing was better than that of the acyclovir treatment group, with reduced scar formation and better skin repair. [4]
Disease Modeling Protocol	Cholestatic hepatitis model Modeling Mechanism： Lithocholic acid, as a highly toxic secondary bile acid, induces hepatocyte apoptosis and necrosis by activating the death receptor (Fas) pathway and disrupting mitochondrial function. At the same time, it inhibits the nuclear receptor (CAR/PXR)-mediated detoxification pathway, leading to liver inflammation, cholestasis, and liver function damage. Related Products： Lithocholic acid (T2202) Modeling Method： Experimental Subject： Mouse, C57BL/6 (WT), CAR⁻/⁻ (CAR knockout), Male, 10 weeks old Dosage and Administration Route： ① Pre-treatment: CAR agonist (Phenobarbital PB 80 mg/kg, TCPOBOP TC 3 mg/kg) or PXR agonist (PCN 200 mg/kg), Intraperitoneal injection (i.p.), Pre-treatment for 3 days; ② Modelling: 125 mg/kg lithocholic acid, Intraperitoneal injection, Continuous co-administration with pre-treatment agents for 3 days Dosing Frequency and Duration Model： Pre-treatment single dose+modelling twice daily Validation： Liver function indicators: Serum ALT levels were significantly elevated (73-fold higher in the LCA group of WT mice compared to the control group), and the elevation was even more significant in CAR⁻/⁻ mice (113-fold); CAR/PXR activator pretreatment reduced ALT by 94%-97%; Histological indicators: Multifocal necrosis and diffuse vacuolation were observed in liver tissue, with more severe damage in CAR⁻/⁻ mice, and PB/TC/PCN pretreatment completely alleviated the necrosis; Immune and inflammatory indicators: Cleaved caspase 3 (apoptosis marker) was strongly positive in the cytoplasm of hepatocytes in the LCA group, and PARP cleavage was increased. Precautions： All mice were sacrificed 12 hours after modeling, and serum and liver tissue were collected for testing. References：Beilke LD,et,al. Decreased apoptosis during CAR-mediated hepatoprotection against lithocholic acid-induced liver injury in mice. Toxicol Lett. 2009 Jul 10;188(1):38-44.
Kinase Assay	Competitive ligand binding assay.: Ligand binding is performed using lysates from COS-7 cells transfected with expression plasmids for VDR or RXRα. Binding is performed overnight at 4°C in lysate buffer with 0.71 nM (18 Ci/mmol) [3H]1,25(OH)2D3 and bile acid competitor. Unbound [3H]1,25(OH)2D3 is removed by adsorption to dextran-coated charcoal and the supernatant removed for scintillation counting. Ki values are calculated from a computer fit of competition curves from triplicate assays.
Synonyms	3α-Hydroxy-5β-cholanic acid

Chemical Properties

Molecular Weight	376.57
Formula	C₂₄H₄₀O₃
Cas No.	434-13-9
Smiles	[H][C@@]12CC[C@H]([C@H](C)CCC(O)=O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CC[C@]2([H])C[C@H](O)CC[C@]12C
Relative Density.	1.0454 g/cm3 (Estimated)

Storage & Solubility Information

Storage

keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 44 mg/mL (116.84 mM), Sonication is recommended.

DMSO: 49 mg/mL (130.12 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6555 mL	13.2777 mL	26.5555 mL	132.7774 mL
5 mM	0.5311 mL	2.6555 mL	5.3111 mL	26.5555 mL
10 mM	0.2656 mL	1.3278 mL	2.6555 mL	13.2777 mL
20 mM	0.1328 mL	0.6639 mL	1.3278 mL	6.6389 mL
50 mM	0.0531 mL	0.2656 mL	0.5311 mL	2.6555 mL
100 mM	0.0266 mL	0.1328 mL	0.2656 mL	1.3278 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

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10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

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Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

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