Pregnane X Receptor (PXR) Activator

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.

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.

Praeruptorin E is an orally active pyranocoumarin compound. Praeruptorin E can be isolated from the dried roots of Peucedanum praeruptorum Dunn. Praeruptorin E reduces the expression of NF-κB. Praeruptorin E upregulates the expression of PXR and CYP3A4. Praeruptorin E inhibits Th2 cytokines, TNF-α, IL6, MPO, and blocks the Ca²⁺ slow channel. Praeruptorin E promotes pulmonary tissue repair and relaxes porcine coronary artery strips. Praeruptorin E protects mice from lipopolysaccharide- and hydrochloric acid-induced acute lung injury. Praeruptorin E can be used in studies related to asthma and acute lung injury.

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.

Imazalil (Enilconazole) is a fungicide. Imazalil has oral activity and strongly activates mPXR but not mCAR in mouse liver. Imazalil is commonly used to protect various agricultural crops against fungal attack. Imazalil induces developmental abnormalities, gut microbiota dysbiosis, and hepatic metabolism disorder.

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.

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).

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.

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.

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.

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.

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.

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.