Cytochrome P450 Activator

Cholestyramine (Cholestyramine resin) is an orally active bile acid sequestrant. Cholestyramine upregulates the expression of intestinal Apical sodium-dependent bile acid transporter and hepatic Cholesterol 7α-hydroxylase. Cholestyramine induces the expression of intestinal and hepatic cholesterol synthesis genes as well as hepatic lipogenesis genes, and promotes bile acid- and neutral sterol-mediated reverse cholesterol transport. Cholestyramine reduces intestinal cholesterol absorption and induces cholesterol efflux. Cholestyramine is applicable to research related to coronary artery disease, atherosclerotic cardiovascular disease and atherosclerosis.

Potassium 1H-indol-3-yl sulfate is a metabolite of tryptophan, produced by intestinal microorganisms and combined with sulfate in the liver before entering the circulatory system. Potassium 1H-indol-3-yl sulfate is a potent endogenous agonist of the aryl hydrocarbon receptor (AhR) and a urinary toxin. Potassium 1H-indol-3-yl sulfate can be used for research on kidney diseases.

Octocrylene is an organic ultraviolet (UV) filter that absorbs mainly UVB radiation and shorter UVA wavelengths. Octocrylene acts as a partial agonist of PPARγ, which alters the gene transcription profile of lipid metabolism enzymes. In addition, Octocrylene is cytotoxic and genotoxic to human skin fibroblasts and mediates the biosynthesis of estrogens such as estriol in zebrafish larvae, while affecting antioxidant pathways including glutathione transferase and peroxisomes.

Phloracetophenone (2,4,6-trihydroxyacetophenone) is the aglycone part of acetophenone glycoside obtained from Curcuma comosa Roxb, with cholesterol-lowering activity. Phloracetophenone enhances cholesterol 7α-hydroxylase (CYP7A1) activity. Phloracetophenone stimulats bile secretion mediated through Mrp2.

Edelfosine (ET-18-OCH3) is an orally active lipid raft modulator and apoptosis inducer that alters membrane fluidity and preferentially inserts into tumor cell membranes. Edelfosine recruits death receptor ligands (FasL/CD95L, TRAIL) and Bid to lipid rafts to form death-inducing signaling complexes, thereby initiating mitochondria-dependent apoptosis and inducing cytochrome c release. Edelfosine also exerts anti-inflammatory effects, promotes L-Selectin shedding, and causes no gastrointestinal or organ toxicity. In addition, Edelfosine inhibits nucleic acid and protein synthesis in Leishmania donovani and exhibits antiproliferative activity. Edelfosine can be used in research on multiple myeloma, inflammatory bowel diseases (such as ulcerative colitis and Crohn's disease), and visceral leishmaniasis.

FPH1(BRD-6125) increases the number and activity of primary human hepatocytes in vitro and promotes the differentiation of iPS cells towards a hepatic lineage.

PELI1-IN-1 (compound 3d) is a potent inhibitor of PELI1, E3 ubiquitin ligase. PELI1-IN-1 has anti-tumPELI1-IN-1, a Resveratrol (HY-16561) derivative, is an orally active PELI1 Inhibitor (K_d = 8.2 μM). PELI1-IN-1 markedly interrupts the interaction of PELI1 and SNAIL/SLUG, and inhibits the K63-polyubiquitization of SNAIL/SLUG by PELI1, subsequently downregulating the protein levels of epithelial-mesenchymal transition (EMT) effectors SNAIL/SLUG. PELI1-IN-1 significantly reduces the level of SNAIL, SLUG and Vimentin without affecting the PELI1 expression. PELI1-IN-1 targets the FHA domain of PELI1 and disrupts the interaction, leading to the anti-metastasis of TNBC cells in vitro and in vivo. PELI1-IN-1 shows no evident toxicity in vivo.

7H-Dibenzo[c,g]carbazole (DBC) is an azaarene with high lipophilicity. 7H-Dibenzo[c,g]carbazole has carcinogenic activity and induce DNA adducts in fish, DNA adducts, mutations in diploid human fibroblasts and micronuclei in human blood lymphocytes. 7H-Dibenzo[c,g]carbazole is activated by cytochrome P450 enzymes resulting mainly in the generation of phenolic metabolites.

Avatrombopag (AKR-501) maleate is an orally active, non-peptide thrombopoietin receptor (TPO receptor) agonist (EC₅₀: 3.3 nM). Avatrombopag maleate mimics the biological activity of TPO. Avatrombopag maleate increases platelet production by activating intracellular signaling systems and promotes the production of platelets and megakaryocytes from hematopoietic precursor cells. Avatrombopag maleate is a substrate for cytochrome P450 (CYP) 2C9 and CYP3A .

MCPA is an orally active phenoxyacetic acid herbicide. MCPA interferes with membrane integrity, energy metabolism (decreases ATP levels), and redox balance in plant cells. MCPA increases hepatic cytochrome P-450 levels and increases aniline hydroxylase and 7-ethoxycoumarin O-deethylase activities. MCPA can be used to control broadleaf weeds.

Potassium 1H-indol-3-yl sulfate-d₄ potassium is the deuterium labeled Potassium 1H-indol-3-yl sulfate. Potassium 1H-indol-3-yl sulfate is a metabolite of tryptophan, produced by intestinal microorganisms and combined with sulfate in the liver before entering the circulatory system. Potassium 1H-indol-3-yl sulfate is a potent endogenous agonist of the aryl hydrocarbon receptor (AhR) and a urinary toxin. Potassium 1H-indol-3-yl sulfate can be used for research on kidney diseases.

GSK2945 hydrochloride is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC₅₀s of 21.5 μM and 20.8 μM, respectively. GSK2945 hydrochloride enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.

(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.

Fipronil (Standard) is the analytical standard of Fipronil. This product is intended for research and analytical applications. Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC₅₀s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes.

1-Hydroxypyrene-d₉ is the deuterium labeled 1-Hydroxypyrene (HY-W014075). 1-Hydroxypyrene, a biomarker of exposure to polycyclic aromatic hydrocarbons (PAHs), is analyzed in urine samples. 1-Hydroxypyrene is the major biomarker of exposure to pyrenes. 1-Hydroxypyrene is the orally active agonist for aryl hydrocarbon receptor (AhR) and can lead to renal fibrosis.

MCPA-d₃ is the deuterium labeled MCPA (HY-B0859). MCPA is an orally active phenoxyacetic acid herbicide. MCPA interferes with membrane integrity, energy metabolism (decreases ATP levels), and redox balance in plant cells. MCPA increases hepatic cytochrome P-450 levels and increases aniline hydroxylase and 7-ethoxycoumarin O-deethylase activities. MCPA can be used to control broadleaf weeds.

Fipronil-¹³C₆ is the ¹³C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.

Monoethyl phthalate-d₄ is the deuterium labeled Monoethyl phthalate. Monoethyl phthalate is an orally active PDX-1 activator and the major hydrolytic metabolite of Diethyl phthalate (HY-Y0284) in vivo, with reproductive toxicity. Monoethyl phthalate targets aromatase (aromatase/CYP19A1) and PPAR to induce cell proliferation. The plasma protein binding rate of Monoethyl phthalate in rats and humans is lower than that of Diethyl phthalate. It exhibits significant enterohepatic circulation in rats and mainly accumulates in liver tissues. Monoethyl phthalate shows no estrogenic activity in estrogen-dependent human breast cancer cells. Monoethyl phthalate can be used in studies of reproductive toxicity and related environmental endocrine disruption mechanisms.

CDD3506 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.

CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.