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Results for "

PXR activation

" in MedChemExpress (MCE) Product Catalog:

25

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2

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2

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7

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2

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-W036120
    Benzophenone-2

    2,2′,4,4′-Tetrahydroxybenzophenone

    		 Pregnane X Receptor (PXR) Estrogen Receptor/ERR Others
    Benzophenone-2 (2,2',4,4'-Tetrahydroxybenzophenone) is an endocrine disruptor targeting pregnane X receptor (PXR) and estrogen receptor α (ERα). Benzophenone-2 regulates cytochrome P450 3A (CYP3A) expression by activating PXR. Benzophenone-2 is promising for research of UV filters .
    Benzophenone-2
  • 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
    (3S,5S)-Atorvastatin

    		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-131723
    Pregnenolone 16α-carbonitrile
    4 Publications Verification

    		 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-15371
    Forskolin
    Maximum Cited Publications
    182 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-175264
    MI891

    		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-174300
    Cholic acid-Glu

    		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-123632
    (3S,5S)-Atorvastatin sodium salt

    		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
    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.
    Desmethyl Bosentan
  • HY-15371G
    Forskolin

    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-N0784
    Ginkgolide B
    5+ 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-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 .
    DL5050
  • HY-15371R
    Forskolin (Standard)

    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-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 .
    MI-883
  • HY-N0784R
    Ginkgolide B (Standard)

    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-16561
    Resveratrol
    140+ Cited Publications

    trans-Resveratrol; SRT501

    		 IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Antibiotic Keap1-Nrf2 Infection Inflammation/Immunology Cancer
    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-119459
    Fluopyram
    1 Publications Verification

    		 Pregnane X Receptor (PXR) Succinate Dehydrogenase Fungal Parasite Constitutive Androstane Receptor Caspase NF-κB 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-W709413
    Panaxytriol

    		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-16561R
    Resveratrol (Standard)
    140+ 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-16561S1
    Resveratrol-13C6

    trans-Resveratrol-13C6; SRT501-13C6

    		 Isotope-Labeled Compounds 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-16561S
    Resveratrol-d4

    trans-Resveratrol-d4; SRT501-d4

    		 Isotope-Labeled Compounds 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-18612
    MK-7725

    		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) with EC50 values for human and mouse BRS-3 of 3 nM and 22-33 nM, respectively. MK-7725 has high binding activity with human BRS-3, with an IC50 of 1.4 nM. 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-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-16561G
    Resveratrol

    trans-Resveratrol; SRT501

    		 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-119459R
    Fluopyram (Standard)

    		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)

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