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hPXR

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By Targets:	Autophagy (4) Constitutive Androstane Receptor (1) Cytochrome P450 (2) Environmental Pollutants (1) FXR (2) HMG-CoA Reductase (HMGCR) (2) Isocitrate Dehydrogenase (IDH) (1) Pregnane X Receptor (PXR) (5) Reference Standards (2)
By Research Areas:	Cancer (3) Endocrinology (3) Inflammation/Immunology (3) Metabolic Disease (4)

Inhibitors & Agonists

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10912

Fexaramine Maximum Cited Publications 10 Publications Verification	FXR Autophagy	Others
Fexaramine is a potent and selective FXR agonist with an EC₅₀ of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors .

HY-100793

SR12813 5+ Cited Publications GW 485801	Pregnane X Receptor (PXR) HMG-CoA Reductase (HMGCR) Autophagy	Metabolic Disease
SR12813 (GW 485801) is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC₅₀ value of 0.85 μM . SR12813 is also an efficient agonist of human pregnane X receptor (hPXR). SR12813 can strongly bind to hPXR but not to mouse PXR (mPXR) .

HY-124830

SPA70 1 Publications Verification	Others	Cancer
SPA70 is a potent and selective antagonist of human pregnane X receptor (hPXR), with an IC₅₀ of 540 nM (K_i=390 nM). SPA70 can enhance the chemosensitivity of cancer cells .

HY-W587839

4,8-Dioxa-3H-perfluorononanoic acid	Pregnane X Receptor (PXR)	Endocrinology
4,8-Dioxa-3H-perfluorononanoic acid is an ether-substituted polyfluoroalkyl compound and also a ligand of human pregnane X receptor (hPXR), which binds to the ligand-binding domain of hPXR. 4,8-Dioxa-3H-perfluorononanoic acid targets Arg-410, Lys-210, Lys-226, Met-323 and His-327 residues. Its binding process relies on long-range electrostatic interactions, and no significant hydrogen bonds form with hPXR residues. 4,8-Dioxa-3H-perfluorononanoic acid is used as a substitute for PFOA in Germany. 4,8-Dioxa-3H-perfluorononanoic acid is detectable in environmental matrices such as river water near fluoride production plants, accumulates in organisms including grass, deer liver and locusts, and is present in plasma samples of populations in southern Germany .

HY-109568

Lynestrenol	Pregnane X Receptor (PXR)	Inflammation/Immunology Endocrinology
Lynestrenol is a pregnane X receptor (PXR) agonist with the EC₅₀s of 41 and 0.23 μM for hPXR and zfPXR, respectively . Lynestrenol, a synthetic progesteronelike agent possess immunostimulatory properties .

HY-111202

Pyributicarb TSH-888	Environmental Pollutants Cytochrome P450	Inflammation/Immunology
Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).

HY-109568R

Lynestrenol (Standard)	Reference Standards Pregnane X Receptor (PXR)	Inflammation/Immunology Endocrinology
Lynestrenol (Standard) is the analytical standard of Lynestrenol. This product is intended for research and analytical applications. Lynestrenol is a pregnane X receptor (PXR) agonist with the EC50s of 41 and 0.23 μM for hPXR and zfPXR, respectively . Lynestrenol, a synthetic progesteronelike agent possess immunostimulatory properties .

HY-N15216

Ganolucidic acid B	Cytochrome P450	Metabolic Disease
Ganolucidic acid B is a triterpenoid compound found in Ganoderma sinense. Ganolucidic acid B can activate *hPXR*-mediated CYP3A4 expression. Ganolucidic acid B can be used in metabolism-related research .

HY-10912R

Fexaramine (Standard)	FXR Autophagy	Others
Fexaramine (Standard) is the analytical standard of Fexaramine. This product is intended for research and analytical applications. Fexaramine is a potent and selective FXR agonist with an EC50 of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors .

HY-134522

DL5050	Constitutive Androstane Receptor	Metabolic Disease Cancer
DL5050 is a selective and potent human constitutive androstane receptor (hCAR) agonist that does not activate pregnane X receptor (PXR). DL5050 preferentially induces the expression of CYP2B6 (target of hCAR) over CYP3A4 (target of hPXR) on both the mRNA and protein levels. DL5050 can be used for the researches of cancer and metabolic disease, such as diabetes .

HY-120181

AGI-14100	Isocitrate Dehydrogenase (IDH)	Cancer
AGI-14100 is a metabolically stable and orally available mIDH1 inhibitor (IC₅₀=6 nM). The pharmacochemical optimization of AGI-14100 is aimed at eliminating hPXR activation, resulting in the final drug candidate AG-120. AG-120 can be used in the study of cancers carrying IDH1 mutations. The discovery and development of AGI-14100 can be used for further studies of mutant isocitrate dehydrogenase 1 (mIDH1) inhibitors .

HY-100793R

SR12813 (Standard) GW 485801 (Standard)	Pregnane X Receptor (PXR) HMG-CoA Reductase (HMGCR) Reference Standards Autophagy	Metabolic Disease
SR12813 (Standard) is the analytical standard of SR12813 (HY-100793). This product is intended for research and analytical applications. SR12813 (GW 485801) is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC50 value of 0.85 μM . SR12813 is also an efficient agonist of human pregnane X receptor (hPXR). SR12813 can strongly bind to hPXR but not to mouse PXR (mPXR) .

Ganolucidic acid B	Triterpenes Microorganisms Terpenoids Source Classification	Cytochrome P450
Ganolucidic acid B is a triterpenoid compound found in Ganoderma sinense. Ganolucidic acid B can activate *hPXR*-mediated CYP3A4 expression. Ganolucidic acid B can be used in metabolism-related research .

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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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hPXR

Inhibitors & Agonists

NaturalProducts

Natural
Products