Lithocholic acid - Moligand™, 10mM in DMSO , Agonist of Farnesoid X receptor;Agonist of GPBA receptor;Agonist of Pregnane X receptor;Agonist of Vitamin D receptor, CAS No.434-13-9, Agonist of Farnesoid X receptor;Agonist of GPBA receptor;Agonist of Pregnane X receptor;Agonist of Vitamin D receptor

CAS: 434-13-9 Cat. No.: L408630 Formula: C₂₄H₄₀O₃ Molecular Weight: 376.57 Beilstein Registry Number: 3217757 EC Number: 207-099-1

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Cholan-24-oic acid, 3-hydroxy-, (3α,5β)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Lithocholic acid Lithocholic acid is a toxic secondary bile acid, causes intrahepatic cholestasis, has tumor-promoting activity, its toxic effect can be protected after it activates the vitamin D receptor , PXR and FXR .
In vitro

Lithocholic acid (LCA) is a hydrophobic secondary bile acid that is primarily formed in the intestine by the bacterial 7α-dehydroxylation of chenodeoxycholic acid. LCA causes intrahepatic cholestasis (cessation or impairment of bile flow). LCA activates PXR (pregnane X receptor), and the LCA-induced severe liver damage can be protected by the activation of PXR. LCA is a ligand for farnesoid X receptor (FXR) with EC50 of 3.8 μM. LCA directly binds VDR (vitamin D receptor) with K_i of 29μM, activates VDR (vitamin D receptor) 30 μM, with much more sensitivity than the other nuclear receptors (eg. PXR, FXR), and its toxic effect is thus protected. LCA has tumor-promoting activity, inhibits mammalian DNA Polymerase β with IC50 of 15 μM.

In vivo

Administration of LCA and its conjugates to rodents causes intrahepatic cholestasis,a pathogenic state characterized by decreased bile flow and the accumulation of bile constituents in the liver and blood. In DMH (dimethyldydrazine)-induced murine carcinogenesis model, LCA suppresses apoptosis almost completely in premalignant colon. LCA activates VDR, induces expression in vivo of CYP3A, a cytochrome P450 enzyme that detoxifies LCA in the liver and intestine.
Cell Data

cell lines：

Concentrations：~30 μM

Incubation Time：Incubation Time:

Powder Purity:≥100%

Specifications

Synonyms

Cholan-24-oic acid, 3-hydroxy-, (3α,5β)-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Lithocholic acid is a toxic secondary bile acid, causes intrahepatic cholestasis, has tumor-promoting activity, its toxic effect can be protected after it activates the vitamin D receptor, PXR and FXR.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

AGONIST

Mechanism of action

Agonist of Farnesoid X receptor;Agonist of GPBA receptor;Agonist of Pregnane X receptor;Agonist of Vitamin D receptor

Names and Identifiers

Isomeric SMILES

C[C@H](CCC(=O)O)[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CC[C@H]4[C@@]3(CC[C@H](C4)O)C)C

WGK Germany

2

RTECS

FZ2275000

Molecular Weight

376.57

Beilstein

3217757

Reaxy-Rn

2818923

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=2818923&ln=

Associated Targets(Human)

VDR Tclin Vitamin D3 receptor (1 Activities)

Discover Target: VDR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NR1H4 Tclin Bile acid receptor (1 Activities)

Discover Target: NR1H4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NR1I2 Tchem Nuclear receptor subfamily 1 group I member 2 (1 Activities)

Discover Target: NR1I2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GPBAR1 Tchem G-protein coupled bile acid receptor 1 (1 Activities)

Discover Target: GPBAR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro
• Specific Rotation[α]: 35.5°
• Melt Point(°C): 183-188°C

Frequently Asked Questions

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 434-13-9, the molecular formula is C24H40O3, and the molecular weight is 376.57 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.