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PXR activation

" in MedChemExpress (MCE) Product Catalog:

35

Inhibitors & Agonists

2

Fluorescent Dyes

2

Biochemical Assay Reagents

11

Natural
Products

2

Isotope-Labeled Compounds

2

GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15371
    Forskolin
    Maximum Cited Publications
    210 Publications Verification

    Coleonol; Colforsin; HL 362

    Organoid Adenylate Cyclase FXR Autophagy PKC Metabolic Disease Inflammation/Immunology Endocrinology Cancer
    Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase . Forskolin is also an inducer of intracellular cAMP formation . Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR . Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy .
    Forskolin
  • HY-16561
    Resveratrol
    155+ Cited Publications

    trans-Resveratrol; SRT501

    DNA/RNA Synthesis IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Antibiotic Keap1-Nrf2 Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Resveratrol (trans-Resveratrol; SRT501) is a CNS-penetrant natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
    Resveratrol
  • HY-N0784
    Ginkgolide B
    10+ Cited Publications

    BN-52021

    Platelet-activating Factor Receptor (PAFR) Apoptosis Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    Ginkgolide B (BN-52021), a terpene lactone, is a potent platelet activating factor antagonist. Ginkgolide B protects endothelial cells via the activation of PXR from injuries induced by xeno- and endobiotics. Ginkgolide B can pass through the brain-blood barrier. Ginkgolide B has anti-oxidant, anti-inflammatory, anti-tumor, and anti-apoptotic activity. Ginkgolide B has marked neuroprotective effects against ischemia-induced impairments .
    Ginkgolide B
  • HY-131723
    Pregnenolone 16α-carbonitrile
    5+ Cited Publications

    Pregnane X Receptor (PXR) Cytochrome P450 Metabolic Disease
    Pregnenolone 16α-carbonitrile is an orally active prototypical and effective rodent-PXR activator. Pregnenolone 16α-carbonitrile, a synthetic steroid, induces cytochrome P450 3A expression. Pregnenolone 16α-carbonitrile exhibits increased resistance to subsequent stressful insults .
    Pregnenolone 16α-carbonitrile
  • HY-119459
    Fluopyram
    1 Publications Verification

    Environmental Pollutants Constitutive Androstane Receptor Parasite Caspase Fungal NF-κB Succinate Dehydrogenase Pregnane X Receptor (PXR) Infection Cancer
    Fluopyram is an orally active succinate dehydrogenase inhibitor, antifungal and nematicide. Fluopyram inhibits succinate dehydrogenase activity, activates CAR/PXR nuclear receptors, and increases caspase-3, TNF-α and NF-κB. Fluopyram inhibits the growth of F. virguliforme, Botrytis cinerea and Alternaria solani with EC50 values of 3.35, 5.389 and 0.244 µg/mL, respectively. Fluopyram induces liver and thyroid tumor formation. Fluopyram is nephrotoxic and embryotoxic .
    Fluopyram
  • HY-16561R
    Resveratrol (Standard)
    155+ Cited Publications

    trans-Resveratrol (Standard); SRT501 (Standard)

    Reference Standards IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Antibiotic Keap1-Nrf2 Infection Inflammation/Immunology Cancer
    Resveratrol (Standard) is the analytical standard of Resveratrol. This product is intended for research and analytical applications. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
    Resveratrol (Standard)
  • 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 .
    TTA-A2
  • HY-16561S

    trans-Resveratrol-d4; SRT501-d4

    Isotope-Labeled Compounds DNA/RNA Synthesis IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Antibiotic Keap1-Nrf2 Infection Inflammation/Immunology Cancer
    Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
    Resveratrol-d4
  • HY-N6023

    Cytochrome P450 Pregnane X Receptor (PXR) Others
    Thermopsoside is a CYP450 isoenzyme inhibitor and PXR activator. Thermopsoside inhibits CYP3A4, CYP2C19, CYP2D6 and CYP2C9 with IC50 values of 6.0 μM, 9.5 μM, 12.0 μM and 32.0 μM, respectively .
    Thermopsoside
  • HY-15371R

    Coleonol (Standard); Colforsin (Standard); HL 362 (Standard)

    Organoid Reference Standards Adenylate Cyclase FXR Autophagy PKC Metabolic Disease Inflammation/Immunology Endocrinology Cancer
    Forskolin (Standard) is the analytical standard of Forskolin. This product is intended for research and analytical applications. Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase . Forskolin is also an inducer of intracellular cAMP formation . Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR . Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy .
    Forskolin (Standard)
  • HY-N4246

    Aquaporin PKC Akt PI3K Apoptosis Monoamine Oxidase Pregnane X Receptor (PXR) Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    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
  • HY-110249
    CINPA1
    1 Publications Verification

    Constitutive Androstane Receptor Metabolic Disease
    CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function .
    CINPA1
  • HY-B0589C

    Cytochrome P450 Metabolic Disease
    (3S,5S)-Atorvastatin is a inactive enantiomer of Atorvastatin. (3S,5S)-Atorvastatin can activate pregnane X receptor (PXR). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids .
    (3S,5S)-Atorvastatin
  • HY-15371G

    Coleonol; Colforsin; HL 362

    Adenylate Cyclase FXR Autophagy PKC Metabolic Disease Inflammation/Immunology Endocrinology Cancer
    Forskolin (Coleonol) (GMP) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase . Forskolin (GMP) is also an inducer of intracellular cAMP formation . Forskolin (GMP) induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR . Forskolin (GMP) exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin (GMP) also induces autophagy .
    Forskolin
  • HY-119459R

    Reference Standards Succinate Dehydrogenase Fungal Parasite Constitutive Androstane Receptor Caspase NF-κB Infection Cancer
    Fluopyram (Standard) is the analytical standard of Fluopyram (HY-119459). This product is intended for research and analytical applications. Fluopyram is an orally active succinate dehydrogenase inhibitor, antifungal and nematicide. Fluopyram inhibits succinate dehydrogenase activity, activates CAR/PXR nuclear receptors, and increases caspase-3, TNF-α and NF-κB. Fluopyram inhibits the growth of F. virguliforme, Botrytis cinerea and Alternaria solani with EC50 values of 3.35, 5.389 and 0.244 µg/mL, respectively. Fluopyram induces liver and thyroid tumor formation. Fluopyram is nephrotoxic and embryotoxic .
    Fluopyram (Standard)
  • HY-W020788

    CGA 154281

    Environmental Pollutants Glutathione S-transferase Estrogen Receptor/ERR Pregnane X Receptor (PXR) FXR Metabolic Disease Cancer
    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-N0784R

    BN-52021 (Standard)

    Reference Standards Platelet-activating Factor Receptor (PAFR) Apoptosis Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    Ginkgolide B (Standard) is the analytical standard of Ginkgolide B. This product is intended for research and analytical applications. Ginkgolide B (BN-52021), a terpene lactone, is a potent platelet activating factor antagonist. Ginkgolide B protects endothelial cells via the activation of PXR from injuries induced by xeno- and endobiotics. Ginkgolide B can pass through the brain-blood barrier. Ginkgolide B has anti-oxidant, anti-inflammatory, anti-tumor, and anti-apoptotic activity. Ginkgolide B has marked neuroprotective effects against ischemia-induced impairments .
    Ginkgolide B (Standard)
  • HY-16561G

    trans-Resveratrol; SRT501

    DNA/RNA Synthesis IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Keap1-Nrf2 Infection Inflammation/Immunology Cancer
    Resveratrol (GMP) is Resveratrol (HY-16561) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
    Resveratrol
  • HY-N9454

    Pregnane X Receptor (PXR) COX NF-κB Amylases β-glucuronidase DNA/RNA Synthesis Amyloid-β NOD-like Receptor (NLR) Pyroptosis Cancer
    Garcinoic acid is an orally active anti-inflammatory agent that crosses the blood-brain barrier. Garcinoic acid also enhances efferocytosis and enzyme/receptor regulation, and selectively inhibits human COX-2, porcine α-amylase, Saccharomyces cerevisiae α-glucosidase and human DNA polymerase β (IC50=11 μM), as well as activates human PXR. Garcinoic acid enhances macrophage efferocytosis via receptors such as MerTK and LRP-1, and promotes the production of pro-resolving lipid mediators. Garcinoic acid inhibits NF-κB activation and pro-inflammatory cytokine secretion, interferes with aggregation, downregulates NLRP3 inflammasome activity, and binds to targets including CD44 and EGFR to inhibit leukemia cell proliferation. The pharmacological activities of Garcinoic acid, such as antioxidant, anti-inflammatory and lipid metabolism-regulating effects, are widely used in studies related to various diseases including atherosclerosis, Alzheimer's disease, type 2 diabetes, inflammatory bowel disease and viral pneumonia .
    Garcinoic acid
  • HY-W709413

    NF-κB TNF Receptor Interleukin Related Pregnane X Receptor (PXR) Constitutive Androstane Receptor Cytochrome P450 Neurological Disease
    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-175264

    Pregnane X Receptor (PXR) Cytochrome P450 Metabolic Disease
    MI891 is a highly selective PXR antagonist (IC50 = 3.76 μM, Kd = 1.7 μM) and inverse agonist (IC50 = 6.1 μM). MI891 selectively disrupts the interaction between PXR and its coactivator SRC1. MI891 effectively inhibits Rifampicin (HY-B0272)-induced PXR activation. MI891 is useful for the study of metabolic diseases and other diseases .
    MI891
  • HY-173033

    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 .
    MI-883
  • HY-18612

    Bombesin Receptor Metabolic Disease
    MK-7725 is a selective, orally active, and blood-brain barrier-permeable agonist of the subtype 3 of the frog skin peptide receptor (BRS-3). MK-7725 has a high affinity for the human BRS-3 (hBRS-3), with an IC50 of 3 nM, and its functional activity in the mouse-derived BRS-3 (mBRS-3) model with an EC50 of 22 nM (105% agonistic). MK-7725 significantly reduces the body weight of obese rats and obese dogs. MK-7725 can be used for the treatment of obesity .
    MK-7725
  • HY-16561S1

    trans-Resveratrol-13C6; SRT501-13C6

    Isotope-Labeled Compounds DNA/RNA Synthesis IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Antibiotic Keap1-Nrf2 Infection Inflammation/Immunology Cancer
    Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
    Resveratrol-13C6
  • HY-W020788R

    CGA 154281 (Standard)

    Reference Standards Glutathione S-transferase Estrogen Receptor/ERR Pregnane X Receptor (PXR) FXR Others
    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-174300

    Pregnane X Receptor (PXR) Metabolic Disease
    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
  • HY-W023836

    Drug Derivative Pregnane X Receptor (PXR) Others
    4-Chloro-2-(trifluoroacetyl)aniline (Compound 10), an analog of Efavirenz (HY-10572), is a Pregnane X receptor (PXR) ligand. 4-Chloro-2-(trifluoroacetyl)aniline has no PXR activation activity without induction of Cyp3a11 mRNA expression .
    4-Chloro-2-(trifluoroacetyl)aniline
  • HY-123632

    Cytochrome P450 Others
    (3S,5S)-Atorvastatin sodium salt is a pregnane X receptor (PXR) activator and the inactive enantiomer of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor with lipid-lowering capabilities .
    (3S,5S)-Atorvastatin sodium salt
  • HY-145516

    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.
    Desmethyl Bosentan
  • HY-134522

    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 .
    DL5050
  • HY-N4246R

    Reference Standards PKC Akt PI3K Apoptosis Pregnane X Receptor (PXR) Monoamine Oxidase Aquaporin Neurological Disease
    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-124773

    Pregnane X Receptor (PXR) Others
    SJB7 is a pregnane X receptor (PXR) agonist. SJB7 can stabilize the activation function 2 (AF-2) helix in an “inward” position .
    SJB7
  • HY-180918

    Potassium Channel Pregnane X Receptor (PXR) Cancer
    ERG-IN-4 (Compound 12) is an orally active, selective ERG inhibitor with an IC50 of 5.2 μM for hERG. ERG-IN-4 activates PXR. ERG-IN-4 exhibits anticancer activity against MTAP-deleted non-small cell lung cancer .
    ERG-IN-4
  • HY-122163

    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 .
    MK-3901
  • HY-179703

    FXR Inflammation/Immunology
    FXR agonist 15 is a selective, potent and orally active farnesoid X receptor (FXR) agonist with EC50 of 0.76 μM. FXR agonist 15 exhibits no obvious activation on other nuclear receptors including LXRα/β, PXR, PPARα/β/γ, THR-β, with EC50 values all >10 μM. FXR agonist 15 can alleviate steatosis, lobular inflammation, hepatocyte ballooning and liver fibrosis. FXR agonist 15 can be used for the research of nonalcoholic steatohepatitis (NASH) .
    FXR agonist 15

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