2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Pregnane X Receptor (PXR)

Pregnane X Receptor (PXR)

Pregnane X Receptor

Pregnane X Receptor (PXR), a member of the nuclear receptor (NR) superfamily, is a ligand-activated transcription factor that plays a crucial role in the metabolism of xenobiotics and endobiotics in mammals. PXR was first recognized as an exogenous substance receptor regulating metabolizing enzymes and transporters and functioning in detoxification and drug metabolism in the liver. However, further research revealed that PXR acts as an equally important endogenous substance receptor in the metabolism and homeostasis of endogenous substances. PXR is highly distributed in small intestine, liver, rectum, colon and bladder, while its expression in other organs and tissues is either moderate, low or undetectable. PXR can be activated by numerous chemical compounds. Activated PXR, through direct binding to the genomic regions or indirect crosstalk with other transcriptional factors, controls various genes involved in biotransformation, transport, inflammation, oxidative stress and etc.
As a master regulator of xenobiotic response PXR adjusts the expression of many drug metabolizing enzymes (DME), such as cytochrome P450, uridine diphosphate (UDP)-glucuronosyltransferases, sulfotransferases and carboxylesterases. PXR also regulates drug-efflux pumps multi-drug resistance gene 1 (MDR1), MDR2, ATP-binding cassette transporter C 2 (ABCC) and anion-transporting polypeptide 2 (OATP). PXR is participated in tumor cell proliferation and growth, apoptosis and metastasis as well as in liver regeneration and hepatic proliferation, indicating the important role of PXR in cancer[1][2].

Pregnane X Receptor (PXR) Related Products (39):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-169280
    PXR Ligand 2
    		Ligand
    PXR Ligand 2 (Compound 55) is the target protein ligand for PROTAC SMARCA2/4-degrader-34 (HY-169279).
    PXR Ligand 2
  • HY-175268
    PXR ligand-Linker Conjugate 1
    PXR ligand-Linker Conjugate 1 is a conjugate of PXR ligand and linker, which can be used to synthesize PROTAC MI1013 (HY-175266).
    PXR ligand-Linker Conjugate 1
  • HY-175267
    PXR Ligand 3
    PXR Ligand 3 is a PXP ligand. PXR Ligand 3 can be used to synthesize PROTAC MI1013 (HY-175266).
    PXR Ligand 3
  • HY-169264
    SJYHJ-026
    		Degrader
    SJYHJ-026 (compound 37) is a pregnane X receptor (PXR) PROTAC degrader with the DC50 of 86.6 nM and maximal degradation of 66.4%. SJYHJ-026 shows cell cytotoxic aganist SNU-C4 HiBiT-PXR KI cells with the IC50 values of 97.4 μM (24 h) and 99.5 μM (72 h) (Blue: VHL ligand HY-125845,Black: linker HY-43048；Pink: PXR inhibitor HY-169277).
    SJYHJ-026
  • HY-N4246R
    Bacopaside I (Standard)
    		Chemical
    Bacopaside I (Standard) is the analytical standard of Bacopaside I. This product is intended for research and analytical applications. Bacopaside I is an orally active aquaporin AQP1 inhibitor and PKC modulator with neuroprotective and anticancer activities. Bacopaside I specifically blocks the water channel and cGMP-gated ion channel activities of AQP1 without affecting AQP4, thereby inhibiting the migration of colon cancer cells expressing AQP1. Bacopaside I activates the Akt pathway by interacting with PI3K, specifically inhibits MAO-A, effectively alleviates neuron necrosis and apoptosis induced by oxygen-glucose deprivation, reduces oxidative stress, and regulates the surface expression of neuroreceptors. When combined with Bacopaside II (HY-N6016), Bacopaside I significantly reduces the viability, proliferation and invasion ability of breast cancer cells, and binds to the pregnane X receptor (PXR). Bacopaside I is applicable to the research of colon cancer, breast cancer, vascular dementia, cerebral ischemia and other related diseases.
    Bacopaside I (Standard)
  • HY-W709413
    Panaxytriol
    		Activator
    Panaxytriol is an active component of ginseng. Panaxytriol inhibits the nuclear translocation of NF-κB, thereby reducing the production of pro-inflammatory factors (such as TNF-α, IL-1β, IL-6) and nitric oxide (NO) induced by LPS (HY-D1056). Panaxytriol upregulates CYP3A4 by activating the nuclear receptor PXR/CAR. Panaxytriol improves motor dysfunction in a mouse model of brain inflammation. Panaxytriol can be used in the research of neurodegenerative diseases (such as Alzheimer's disease).
    Panaxytriol
  • HY-109568R
    Lynestrenol (Standard)
    		Agonist
    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.
    Lynestrenol (Standard)
  • HY-169277
    PXR Ligand 1
    		Ligand
    PXR Ligand 1 is a PXR Ligand and can be used for synthesis of SJYHJ-026 (HY-169264) PROTACs.
    PXR Ligand 1
  • HY-W020788
    Benoxacor
    		Activator 99.39%
    Benoxacor (CGA 154281) is a herbicide safener and xenobiotic metabolism regulator. Benoxacor protects maize from the toxicity of metolachlor mainly by inducing detoxifying enzymes such as Glutathione S-transferase. Benoxacor also activates FXR, PXR and ERRα, and inhibits aromatase (aromatase). However, Benoxacor exhibits potential subacute oral toxicity and a high risk of hepatotoxicity in animal models. Benoxacor induces reactive oxygen species accumulation, interferes with embryonic heart development, and causes increased liver and kidney weights as well as alterations in gut microbiota in mice. Benoxacor can be used in studies related to hepatic steatosis, infertility, breast cancer and developmental toxicity.
    Benoxacor
  • HY-124773
    SJB7
    		Agonist
    SJB7 is a pregnane X receptor (PXR) agonist. SJB7 can stabilize the activation function 2 (AF-2) helix in an “inward” position.
    SJB7
  • HY-169279
    PROTAC SMARCA2/4-degrader-34
    		Degrader
    PROTAC SMARCA2/4-degrader-34 (compound 38) is a potent is a potent SMARCA2 and SMARCA4 PROTAC degrader. PROTAC SMARCA2/4-degrader-34 shows PXR binding affinity with DC50 value of 85.1 nM. PROTAC SMARCA2/4-degrader-34 decreases the protein expression of 3xFLAG-PXR. (Pink: Ligand for target protein (HY-169280); Black: Linker (HY-43048); Blue: Ligand for E3 ligase (HY-125845).
    PROTAC SMARCA2/4-degrader-34
  • HY-176967
    N-Cholyl-L-glutamic acid
    		Activator
    N-Cholyl-L-glutamic acid (GluCA) is a Cholic acid (HY-N0324) conjugated with L-glutamic acid (HY-14608). N-Cholyl-L-glutamic acid increases expression of PXR and downstream PXR-target gene Cyp3a11. N-Cholyl-L-glutamic acid can be used in the research of Crohn's disease.
    N-Cholyl-L-glutamic acid
  • HY-176965
    N-Cholyl-L-threonine
    		Agonist
    N-Cholyl-L-threonine (ThrCA) is a Cholic acid (HY-N0324) conjugated with L-threonine (HY-N0658). N-Cholyl-L-threonine possesses PXR agonism activity. N-Cholyl-L-threonine can be used in the research of Crohn's disease.
    N-Cholyl-L-threonine
  • HY-169320
    SJPYT-328
    		Agonist
    SJPYT-328 is a PXR agonsit. PXR plays a major role in drug metabolism and drug-drug interactions.
    SJPYT-328
  • HY-100793R
    SR12813 (Standard)
    		Agonist
    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).
    SR12813 (Standard)
  • HY-W020788R
    Benoxacor (Standard)
    		Activator
    Benoxacor (Standard) is the analytical standard of Benoxacor. This product is intended for research and analytical applications. Benoxacor (CGA 154281) is a herbicide safener and xenobiotic metabolism regulator. Benoxacor protects maize from the toxicity of metolachlor mainly by inducing detoxifying enzymes such as Glutathione S-transferase. Benoxacor also activates FXR, PXR and ERRα, and inhibits aromatase (aromatase). However, Benoxacor exhibits potential subacute oral toxicity and a high risk of hepatotoxicity in animal models. Benoxacor induces reactive oxygen species accumulation, interferes with embryonic heart development, and causes increased liver and kidney weights as well as alterations in gut microbiota in mice. Benoxacor can be used in studies related to hepatic steatosis, infertility, breast cancer and developmental toxicity.
    Benoxacor (Standard)
  • HY-B1134A
    Imazalil sulfate
    		Activator 99.63%
    Imazalil (Enilconazole) sulfate is a fungicide. Imazalil sulfate has oral activity and strongly activates mPXR but not mCAR in mouse liver. Imazalil sulfate is commonly used to protect various agricultural crops against fungal attack. Imazalil sulfate induces developmental abnormalities, gut microbiota dysbiosis, and hepatic metabolism disorder.
    Imazalil sulfate
  • HY-148223
    Tolindate
    		Agonist
    Tolindate is a potent PXR agonist with an EC50 value of 8.3 μM. Tolindate shows antifungal activity.
    Tolindate
  • HY-174300
    Cholic acid-Glu
    		Activator
    Cholic acid-Glu is a derivative of Cholic acid (HY-N0324). The abundance of Cholic acid-Glu is increased in Crohn’s disease. Cholic acid-Glu increases PXR activation and significantly increases the expression of the downstream PXR target gene Cyp3a11 in small intestinal organoid tissue.
    Cholic acid-Glu