Cytochrome P450 Modulator

PIPE-791 is an orally active, blood-brain barrier-permeable selective antagonist of LPAR1. PIPE-791 inhibits LPA-induced calcium mobilization, collagen expression, histamine release, and the activation of fibroblasts, microglia and macrophages. PIPE-791 induces oligodendrocyte precursor cell differentiation, myelination and remyelination, and increases the number of microglia in the retina of normotensive rats. PIPE-791 protects mature oligodendrocytes from cytokine-induced death, reduces the levels of pulmonary fibrosis markers and alleviates neuroinflammation in preclinical models. PIPE-791 can be used in the research of glaucoma, neuroinflammatory diseases, chronic osteoarthritis pain, idiopathic pulmonary fibrosis and multiple sclerosis.

Chlorzoxazone is a SK-type potassium channel activator. Chlorzoxazone modulates FOXO3 phosphorylation and Aβ. Chlorzoxazone enhances immunosuppression, attenuates vasoconstriction, attenuates cognitive deficits, and improves experimental autoimmune encephalomyelitis.

TGFBR1-IN-2 (Compound AQA) is a TGFBR1 inhibitor and an antibacterial agent. TGFBR1-IN-2 is a substrate for cytochrome P450s. TGFBR1-IN-2 contains the pyridyl-6-methyl moiety necessary for Mycobacterium tuberculosis inhibition and has potent inhibitory activity against non-replicating and persistent Mycobacterium tuberculosis.

Mancozeb is a widely used fungicide that is effective against fungal diseases in most cereals, vegetables, fruits and ornamental plants. In addition, Mancozeb can cause liver damage in mice by activating the Keap1/Nrf2 signaling pathway. Mancozeb upregulates lactate dehydrogenase and cytochrome c to alter cell metabolism and induce cell death. Mancozeb has reproductive toxicity and can induce apoptosis in ovarian cells.

m-Tolualdehyde (3-Methylbenzaldehyde) is an aldehyde metabolite produced by m-xylene metabolism, and it bidirectionally regulates the CYP 2B1, CYP 2E1, and CYP 4B1 isoenzymes in the respiratory tract of rats. m-Tolualdehyde serves as an oxidation substrate and carbon source for Pseudomonas Pxy, and it can be oxidized to m-toluic acid in an NAD⁺ -dependent manner. m-Tolualdehyde exerts a dose-dependent inhibitory effect on CYP 2B1 and CYP 2E1 in the nasal mucosa and lungs of rats, and a dose-dependent activating effect on pulmonary CYP 4B1. m-Tolualdehyde can form aldehyde-heme adducts with the heme group of cytochrome P450. m-Tolualdehyde can be used in studies related to metabolic enzymes in the respiratory tract of rats.

Chlorzoxazone (Standard) is the analytical standard of Chlorzoxazone. This product is intended for research and analytical applications.

N-Desmethyl-Apalutamide, the major active metabolite of Apalutamide (HY-16060), is a selective competitive inhibitor of androgen receptor. N-Desmethyl-Apalutamide is catalyzed by CYP3A4 and CYP2C8 enzymes. The plasma protein binding rate of N-Desmethyl-Apalutamide reaches 95%, with albumin as the primary binding protein. N-Desmethyl-Apalutamide is suitable for prostate cancer-related research.

Chlorzoxazone-d₃ is the deuterium labeled Chlorzoxazone. Chlorzoxazone is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort. It acts on the spinal cord by depressing reflexes.Chlorzoxazone is currently being used as a marker substrate in vitro/vivo studies to quantify cytochrome P450 2E1 (CYP2E1) activity in humans.

MI-883 is orally active constitutive androstane receptor (CAR) (EC₅₀ of 73 nM) agonist and pregnane X Receptor (PXR) (IC₅₀ of 100 nM) antagonist. MI-883 binds to CAR and PXR ligand-binding domains, promotes CAR LBD assembly, activates CAR3 variant, stimulates CAR cytoplasmic-nuclear translocation, upregulates CAR target genes, recruits coactivators NCOA1, NCOA2, NCOA3, inhibits basal and agonist-induced PXR activation, downregulates PXR target genes, disrupts PXR-NCOR2 interaction, blocks agonist-mediated PXR-NCOA1 recruitment. MI-883 reduces plasma total cholesterol, LDL cholesterol, and hepatic free cholesterol levels, increases fecal bile acid excretion, regulates genes involved in xenobiotic metabolism, cholesterol homeostasis, and bile acid homeostasis. MI-883 exhibits metabolic stability, liver-predominant distribution, a safety profile with no observed toxicity, and does not stimulate human hepatocyte hypertrophy or hyperplasia. MI-883 can be used for the research of diet-induced hypercholesterolemia.

(R)-Esomeprazole ((R)-Omeprazole; (+)-Omeprazole) is an orally active cytochrome P450 2C19, CYP3A4, and CYP2C9-related metabolic modulator. (R)-Esomeprazole can be used in studies of digestive system diseases and compound metabolic interactions.

Flu-6 is a metabolite of Flutamide (HY-B0022). FLU-6 production in the liver requires the involvement of NADPH: cytochrome P450 reductase (CPR). Flutamide can inhibit prostate cancer progression.

Benzylurea is an anti-inflammatory agent. Benzylurea inhibits LPS (HY-D1056)-induced upregulation of MTCH2 expression and regulates pathways associated with mitochondrial function, inflammation and cell survival. Benzylurea alleviates LPS-induced proliferation inhibition and apoptosis of periodontal ligament fibroblasts, as well as the release of proinflammatory cytokines. Benzylurea can be used in studies related to periodontitis.

ZSTK3744 hydrochloride is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 hydrochloride directly binds to AhR, upregulates the expression of AhR target genes including CYP1A1, CYP1B1 and TIPARP, and mediates cell growth inhibitory activity in triple-negative breast cancer cells. ZSTK3744 hydrochloride induces apoptosis in triple-negative breast cancer cells. ZSTK3744 hydrochloride exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer.

ZSTK3744 is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 directly binds to AhR, upregulates the expression of AhR target genes including CYP1A1, CYP1B1 and TIPARP, and mediates cell growth inhibitory activity in triple-negative breast cancer cells. ZSTK3744 induces apoptosis in triple-negative breast cancer cells. ZSTK3744 exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer.

Bitertanol (Biloxazol) is a potent antifungal agent. Bitertanol also is an CYP1A1, CYP2B, and CYP3A inducer in vivo and an CYP1A inhibitor in vitro.

Anticancer agent 310 is an antitumor agent. Anticancer agent 310 releases nitric oxide to induce mitochondrial ROS burst, triggers mitochondrial dysfunction and activates the Bax/Bcl-2-Cyt c-Caspase-9/Caspase-3 apoptotic pathway. Anticancer agent 310 also reduces the levels of SHMT2 and MTHFD2, decreases the ratios of NADPH/NADP⁺ and GSH/GSSG, thereby disrupting redox homeostasis and exacerbating intracellular ROS accumulation. Anticancer agent 310 can be used in research related to gastric cancer.

Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance.

N-Desmethyl-Apalutamide-15N,d4 is the ¹⁵N and deuterium labeled isotope of N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl-Apalutamide, the major active metabolite of Apalutamide (HY-16060), is a selective competitive inhibitor of androgen receptor. N-Desmethyl-Apalutamide is catalyzed by CYP3A4 and CYP2C8 enzymes. The plasma protein binding rate of N-Desmethyl-Apalutamide reaches 95%, with albumin as the primary binding protein. N-Desmethyl-Apalutamide is suitable for prostate cancer-related research.

Thienyldecyl isothiocyanate is an analog of thienylbutyl isothiocyanate that, like many isothiocyanates, demonstrates antiproliferative activity against cancer cells presumably by modulation of xenobiotic-metabolizing enzymes, such as by inhibition of cytochrome P450, and/or by induction of phase II detoxifying enzymes.

m-Tolualdehyde (Standard) is the analytical standard of m-Tolualdehyde (HY-78086). This product is intended for research and analytical applications. m-Tolualdehyde (3-Methylbenzaldehyde) is an aldehyde metabolite produced by m-xylene metabolism, and it bidirectionally regulates the CYP 2B1, CYP 2E1, and CYP 4B1 isoenzymes in the respiratory tract of rats. m-Tolualdehyde serves as an oxidation substrate and carbon source for Pseudomonas Pxy, and it can be oxidized to m-toluic acid in an NAD⁺ -dependent manner. m-Tolualdehyde exerts a dose-dependent inhibitory effect on CYP 2B1 and CYP 2E1 in the nasal mucosa and lungs of rats, and a dose-dependent activating effect on pulmonary CYP 4B1. m-Tolualdehyde can form aldehyde-heme adducts with the heme group of cytochrome P450. m-Tolualdehyde can be used in studies related to metabolic enzymes in the respiratory tract of rats.