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Lithocholic acid (LCA)

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Drug Derivative (1) Drug Metabolite (1) G protein-coupled Bile Acid Receptor 1 (1) GPR39 (1) Isotope-Labeled Compounds (1) Liposome (1) ROR (2)
By Research Areas:	Cancer (2) Inflammation/Immunology (2) Metabolic Disease (2)

Inhibitors & Agonists

Biochemical Assay Reagents

Peptides

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-113238A

Lithocholic acid 3-sulfate disodium SulfoLithocholic acid disodium; LCAS disodium	GPR39 ROR	Metabolic Disease Inflammation/Immunology
Lithocholic acid 3-sulfate disodium is a GPR39 agonist, with EC₅₀ values of 41 μM and 42.4 μM in M39-20 and hGPR39-2 cells, respectively, in the absence of Zn ²⁺, and 0.88 μM and 0.97 μM in the presence of Zn ²⁺. Lithocholic acid 3-sulfate disodium acts as a RORγt ligand. Lithocholic acid 3-sulfate disodium stimulates the GPR39 receptor to initiate intracellular calcium signaling, independent of the Zn ²⁺-binding sites H17 and H19. LCA-3-S selectively inhibits Th17 cell differentiation by targeting RORγt. Lithocholic acid 3-sulfate disodium can be used in the research of cholestatic liver diseases .

HY-177795

5β-Cholanic acid-3,6-dione 3,6-Diketo-LCA	Drug Derivative	Others
5β-Cholanic acid-3,6-dione (3,6-Diketo-LCA) is a similar substance to Lithocholic acid (LCA) (HY-B0172). 5β-Cholanic acid-3,6-dione cannot activate the Vitamin D receptor (VDR), and can be used as a negative control for studying the relationship between LCA derivatives and VDR .

HY-143712S1

Allolithocholic Acid-d4 3α-hydoxy-5α-Cholaoic acid-d4, allo-LCA-d₄	Isotope-Labeled Compounds Drug Metabolite G protein-coupled Bile Acid Receptor 1 ROR	Metabolic Disease Inflammation/Immunology Cancer
Allolithocholic Acid-d₄ (3α-hydoxy-5α-Cholaoic Acid-d₄, allo-LCA-d₄) is deuterium labeled Allolithocholic acid (HY-143712). Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC₅₀ = 2.7 μM) and RORγt inverse agonist (IC₅₀ = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease .

HY-P11614

LCA-H10	Liposome	Cancer
LCA-H10 is a lithocholic acid-histidine decapeptide conjugate, a biocompatible lipid nanoparticle (LNP) additive that reduces ionizable lipid proportions, functions as an endosomal escape inducer, and enhances siRNA encapsulation. LCA-H10 increases hepatic accumulation of LNPs in mice after intravenous injection when incorporated into LiLNP-LH and reduces proinflammatory cytokines (IL-6, TNF, IL-1β) in mouse serum. LCA-H10 can be used for the research of prostate cancer .

Cat. No.	Product Name	Type

HY-113238A

Lithocholic acid 3-sulfate disodium SulfoLithocholic acid disodium; LCAS disodium	Biochemical Assay Reagents
Lithocholic acid 3-sulfate disodium is a GPR39 agonist, with EC₅₀ values of 41 μM and 42.4 μM in M39-20 and hGPR39-2 cells, respectively, in the absence of Zn ²⁺, and 0.88 μM and 0.97 μM in the presence of Zn ²⁺. Lithocholic acid 3-sulfate disodium acts as a RORγt ligand. Lithocholic acid 3-sulfate disodium stimulates the GPR39 receptor to initiate intracellular calcium signaling, independent of the Zn ²⁺-binding sites H17 and H19. LCA-3-S selectively inhibits Th17 cell differentiation by targeting RORγt. Lithocholic acid 3-sulfate disodium can be used in the research of cholestatic liver diseases .

Lithocholic acid 3-sulfate disodium

SulfoLithocholic acid disodium; LCAS disodium

Biochemical Assay Reagents

Lithocholic acid 3-sulfate disodium is a GPR39 agonist, with EC₅₀ values of 41 μM and 42.4 μM in M39-20 and hGPR39-2 cells, respectively, in the absence of Zn ²⁺, and 0.88 μM and 0.97 μM in the presence of Zn ²⁺. Lithocholic acid 3-sulfate disodium acts as a RORγt ligand. Lithocholic acid 3-sulfate disodium stimulates the GPR39 receptor to initiate intracellular calcium signaling, independent of the Zn ²⁺-binding sites H17 and H19. LCA-3-S selectively inhibits Th17 cell differentiation by targeting RORγt. Lithocholic acid 3-sulfate disodium can be used in the research of cholestatic liver diseases .

Cat. No.	Product Name	Target	Research Area

HY-P11614

LCA-H10	Liposome	Cancer
LCA-H10 is a lithocholic acid-histidine decapeptide conjugate, a biocompatible lipid nanoparticle (LNP) additive that reduces ionizable lipid proportions, functions as an endosomal escape inducer, and enhances siRNA encapsulation. LCA-H10 increases hepatic accumulation of LNPs in mice after intravenous injection when incorporated into LiLNP-LH and reduces proinflammatory cytokines (IL-6, TNF, IL-1β) in mouse serum. LCA-H10 can be used for the research of prostate cancer .

Cat. No.	Product Name	Chemical Structure

HY-143712S1

Allolithocholic Acid-d4
Allolithocholic Acid-d₄ (3α-hydoxy-5α-Cholaoic Acid-d₄, allo-LCA-d₄) is deuterium labeled Allolithocholic acid (HY-143712). Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC₅₀ = 2.7 μM) and RORγt inverse agonist (IC₅₀ = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease .

Allolithocholic Acid-d4

Allolithocholic Acid-d₄ (3α-hydoxy-5α-Cholaoic Acid-d₄, allo-LCA-d₄) is deuterium labeled Allolithocholic acid (HY-143712). Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC₅₀ = 2.7 μM) and RORγt inverse agonist (IC₅₀ = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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