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human pregnane X receptor

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By Targets:	Pregnane X Receptor (PXR) (5) Autophagy (2) Calcium Channel (1) Constitutive Androstane Receptor (2) Cytochrome P450 (5) Drug Metabolite (1) Environmental Pollutants (1) G protein-coupled Bile Acid Receptor 1 (1) HMG-CoA Reductase (HMGCR) (2) Interleukin Related (1) LRRK2 (1) Mps1 (1) NF-κB (1) P2X Receptor (1) Prostaglandin Receptor (1) Reference Standards (1) UGT (1)
By Research Areas:	Cancer (2) Endocrinology (1) Inflammation/Immunology (3) Metabolic Disease (6) Neurological Disease (3)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

Recombinant Proteins

Click Chemistry

Targets Recommended: Pregnane X Receptor (PXR)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100793

SR12813 Maximum Cited Publications 7 Publications Verification 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-111828

TTA-A2 1 Publications Verification	Calcium Channel	Neurological Disease
TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a₁G) and Cav3.2 (a₁H) channels with IC₅₀ values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy .

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-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-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-168328

FKK6	NF-κB Interleukin Related	Inflammation/Immunology
FKK6 is a selective agonist for **pregnane X receptor (PXR) with an EC₅₀** of 1.2 µM. FKK6 exhibits good affinity with plasma proteins, and good metabolic metabolism in human microsomes. FKK6 inhibits PXR-related NF-κB signaling pathway, inhibits the expression of inflammatory factors, and exhibits anti-inflammatory activity against DSS (HY-116282)-induced colitis in mouse model .

HY-173033

MI-883	Pregnane X Receptor (PXR) Constitutive Androstane Receptor Cytochrome P450	Metabolic Disease
MI-883 is the orally active agonist for Constitutive Androstane Receptor (CAR, EC₅₀=73 nM) and the antagonist for **Pregnane X Receptor (PXR, IC₅₀=0.1 μM). MI-883 stimulates CAR LBD assembly (EC₅₀=0.38 µM) and CAR3 variant activation (EC₅₀*=0.074 µM), induces CYP2B6 mRNA expression in HepaRG and primary human* hepatocytes. MI-883 inhibits basal PXR activity IC₅₀=2.03 µM) in transiently transfected HepG2 cells, blocks CYP3A4 mRNA expression in HepG2. MI-883 regulates cholesterol metabolism and bile acid excretion, improves hypercholesterolemia in mouse models .

HY-145516

Desmethyl Bosentan Ro 47-8634	Drug Metabolite Cytochrome P450	Metabolic Disease
Desmethyl bosentan is an active metabolite of the endothelin receptor antagonist bosentan (HY-A0013).1 Desmethyl bosentan (25 μM) activates the pregnane X receptor (PXR) in CV-1 monkey kidney cells expressing the human receptor in a reporter assay.

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-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) .

HY-122163

MK-3901	P2X Receptor UGT Cytochrome P450 Pregnane X Receptor (PXR)	Neurological Disease
MK-3901 is a selective P2X3 receptor antagonist with an IC₅₀ of 24 nM. MK-3901 inhibits UGT1A1 (with an IC₅₀ of 1 μM) and CYP2C9 (with an IC₅₀ of 5.7 μM). MK-3901 activates PXR. MK-3901 induces hyperbilirubinemia. MK-3901 can be used for the research of inflammatory pain .

HY-182637

ACT-774312	Prostaglandin Receptor	Inflammation/Immunology
ACT-774312 is a potent and selective CRTH2 antagonist with an IC₅₀ of 4 nM. ACT-774312 blocks the activity and internalization of the CRTH2 receptor, and inhibits PGD₂-induced morphological changes in eosinophils. ACT-774312 can be used in the research of nasal polyps and type 2 inflammatory diseases.

HY-182582

ZY12201	G protein-coupled Bile Acid Receptor 1 Cytochrome P450	Metabolic Disease
ZY12201 is a selective and orally active TGR5 agonist and pan-CYP inhibitor. ZY12201 lowers glucose levels. ZY12201 induces enzymes regulated through Aryl Hydrocarbon Receptor, Constitutive Androstane Receptor, and Pregnane X Receptor. ZY12201 can be used for the research of type 2 diabetes .

HY-182928

LRRK2-IN-21	LRRK2 Mps1	Neurological Disease
LRRK2-IN-21 is a selective, blood-brain barrier-permeable LRRK2 kinase inhibitor with an IC₅₀ of 0.35 nM. LRRK2-IN-21 inhibits TTK kinase with an IC₅₀ of 70 nM. LRRK2-IN-21 is applicable to the research of Parkinson's disease .

Species:	Human (2)
Tag:	His (1) Tag Free (1)
Source:	E. coli (2)

Cat. No.	Compare	Product Name	Species	Source	Image

HY-P701396

	PXR Protein, Human NR1I2; Nuclear receptor subfamily 1 group I member 2; Orphan nuclear receptor PAR1; Orphan nuclear receptor PXR; pregnane X receptor; Steroid and xenobiotic receptor; SXR	Human	E. coli
	The PXR protein is a nuclear receptor that acts as a multifunctional transcription factor activated by a variety of endogenous and exogenous compounds. It regulates genes involved in the metabolism and secretion of substances, responding to ligands such as rifampicin, hypericin, gugulin, colupulone, isoflavones, pregnenolone and progesterone. PXR Protein, Human is the recombinant human-derived PXR protein, expressed by E. coli , with tag free.

HY-P701397

	PXR Protein, Human (His) NR1I2; Nuclear receptor subfamily 1 group I member 2; Orphan nuclear receptor PAR1; Orphan nuclear receptor PXR; pregnane X receptor; Steroid and xenobiotic receptor; SXR	Human	E. coli
	The PXR protein is a nuclear receptor that acts as a multifunctional transcription factor activated by a variety of endogenous and exogenous compounds. It regulates genes involved in the metabolism and secretion of substances, responding to ligands such as rifampicin, hypericin, gugulin, colupulone, isoflavones, pregnenolone and progesterone. PXR Protein, Human (His) is the recombinant human-derived PXR protein, expressed by E. coli , with N-6*His labeled tag.

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Cat. No.	Product Name		Classification

HY-168328

FKK6		Alkynes
FKK6 is a selective agonist for **pregnane X receptor (PXR) with an EC₅₀** of 1.2 µM. FKK6 exhibits good affinity with plasma proteins, and good metabolic metabolism in human microsomes. FKK6 inhibits PXR-related NF-κB signaling pathway, inhibits the expression of inflammatory factors, and exhibits anti-inflammatory activity against DSS (HY-116282)-induced colitis in mouse model .

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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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