Cytochrome P450 Activator

Quinestrol (Standard) is the analytical standard of Quinestrol (HY-B1012). This product is intended for research and analytical applications. Quinestrol (W-3566) is an orally effective synthetic estrogen compound that acts on CYP3A4, CYP1A2, and GnRH. Quinestrol interferes with GnRH release and disrupts the hypothalamic-pituitary-ovarian axis. Quinestrol downregulates the gene expression of follicle-stimulating hormone β and luteinizing hormone β, induces oxidative stress, damages reproductive organs, reduces sperm density and motility, increases sperm malformation rate, and alters the levels of sex hormones such as testosterone, luteinizing hormone, estradiol, and progesterone. Quinestrol can be used in studies related to reproductive function regulation.

Apoptosis inducer 30 (Compound 15a) is an anticancer agent. Apoptosis inducer 30 induces MCF-7 cells apoptosis through mitochondrial pathway. Apoptosis inducer 30 induces intracellular reactive oxygen species levels and decreases mitochondrial membrane potential, and blocks the cell cycle in the G0/G1 phase. Apoptosis inducer 30 inhibits cell growth, with an IC₅₀ value of 0.32 μM against MCF-7 cells, and inhibits tumor growth in a mouse model of breast cancer.

11-HETE (11-Hydroxy-5,8,12,14-eicosatetraenoic acid) is the activator for cytochrome P450. 11-HETE upregulates the mRNA expressions of CYP1B1, CYP1A1, CYP4A11, CYP4F11, and CYP4F2, induces cell hypertrophy in RL-14 cell, and exhibits potential to be used in cardiovascular diseases.

Methysticin is a major kavalactone in kava extract to induce CYP1A1.

1,2,3,4,7,8-Hexachlorodibenzofuran (1,2,3,4,7,8-HxCDF) promotes the gene expressions of CYP1A1, CYP1B1, and aryl hydrocarbon receptor repressor (AhRR) in human peripheral blood lymphocytes (PBLs). 1,2,3,4,7,8-Hexachlorodibenzofuran activates the ethoxyresorufin-Odeethylase, achieves 20% of the maximum response caused by TCDD with a BMR20TCDD of 0.115-0.143 nM.

Octachlorodibenzo-p-dioxin (OCDD) is an environmental contaminant but is not acutely toxic. In rats, Octachlorodibenzo-p-dioxin (50 μg/kg i.v. or 50-5000 μg/kg p.o.) has a systemic elimination half-life of 3-5 months and accumulates and concentrates in the liver and adipose tissue after low-dose, repeated exposure. Repeated administration of octachlorodibenzo-p-dioxin causes increases in 7-ethoxyresorufin-O-deethylase (7-EROD) activity and total cytochrome P-450 levels.

Potassium 1H-indol-3-yl sulfate (Standard) is the analytical standard of Potassium 1H-indol-3-yl sulfate (HY-W011910). This product is intended for research and analytical applications. 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.

5F-203 (Standard) (NSC-703786 (Standard)) is the analytical standard of 5F-203 (HY-124421). This product is intended for research and analytical applications. 5F-203 (NSC-703786) is an aryl hydrocarbon receptor (AhR) agonist and the active moiety of the water-soluble benzothiazole prodrug Phortress (HY-103223). 5F-203 binds to cytosolic AhR and induces CYP1A1 and CYP1B1 expression. 5F-203 activates AhR signaling to induce DNA damage, cell cycle arrest, apoptosis, caspase-3/-7 activation, lysosomal membrane permeabilization, and Cathepsin B release. 5F-203 induces CYGB and pro-apoptotic protein expression and NAG-1 mRNA/protein induction through RNA stabilization. 5F-203 is used in research related to cancers such as triple-negative breast cancer and colorectal cancer.

Tabersonine hydrochloride is a selective, orally active NLRP3 inhibitor. Tabersonine hydrochloride directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine hydrochloride also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine hydrochloride can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine hydrochloride is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer.

Oxiconazole nitrate (Standard) is the analytical standard of Oxiconazole nitrate. This product is intended for research and analytical applications. Oxiconazole (Ro 13-8996) nitrate is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole nitrate is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole nitrate exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest.

AZD7325 (Standard) is the analytical standard of AZD7325. This product is intended for research and analytical applications. AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.

MCPA-d₃-1 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.

Avatrombopag (maleate) (Standard) is the analytical standard of Avatrombopag (maleate). This product is intended for research and analytical applications. Avatrombopag maleate (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag maleate mimics the biological activities of TPO. Avatrombopag maleate increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag maleate is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A.

FPH1 (Standard) is the analytical standard of FPH1 (HY-100590). This product is intended for research and analytical applications. 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.

Pretilachlor (Standard) is the analytical standard of Pretilachlor (HY-B2035). This product is intended for research and analytical applications. Pretilachlor is a chloroacetamide herbicide with biological activities including endocrine disruption, oxidative stress induction, apoptosis induction, and immunotoxicity. Pretilachlor exerts its effects by interfering with hormone metabolism, inducing oxidative stress, activating apoptotic pathways, and inhibiting immune functions. Pretilachlor upregulates the transcription of P53, Mdm2, and Bbc3, and increases the activities of Caspase3 and Caspase9; it upregulates the transcription of genes in the HPG/HPT axis and the activity of aromatase; it induces oxidative stress, elevates ROS levels, and upregulates CAT, SOD, and GPX. Pretilachlor downregulates the transcription of CXCL-C1C, IL-1β, and IL-8. Pretilachlor disrupts the normal physiological processes and embryonic development of fish, exhibiting significant toxicity. Pretilachlor can be used in studies related to weeding, environmental pollution, and behavioral toxicity in fish.

CDD3505 (Standard) is the analytical standard of CDD3505 (HY-100901). This product is intended for research and analytical applications. CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.

Cilobamine methanesulfonate is an orally active antidepressant and a dopamine/norepinephrine reuptake inhibitor. Cilobamine methanesulfonate increases the levels of Aniline hydroxylase and cytochrome P-450 in rat liver. Cilobamine methanesulfonate promotes hypertrophy of the smooth endoplasmic reticulum in rat liver hepatocytes, increases relative liver weight and recoverable microsomal protein. Cilobamine methanesulfonate produces stimulant and anxiogenic effects, and does not inhibit monoamine oxidase. Cilobamine methanesulfonate can be used in the research of depression.

Herbicide safener-4 is a herbicide safener targeting acetolactate synthase (ALS). Herbicide safener-4 competitively binds to the active site of ALS, blocks the binding of Mesosulfuron-methyl (HY-126987), and simultaneously allows substrates to enter for catalytic reactions. Herbicide safener-4 increases the content/activity of glutathione (GSH), glutathione S-transferase (GST), cytochrome P450 monooxygenase (CYP450) and peroxidase (POD) in plants, and decreases the activity of superoxide dismutase (SOD).

Sudan IV-d₆ (Solvent Red 24-d₆) is the deuterium labeled Sudan IV(HY-D0932). Sudan IV is an agonist of the aryl hydrocarbon receptor (AhR) that activates downstream signaling pathways and induces CYP1A1 expression. Sudan IV promotes CYP1A1 gene transcription by activating AhR-ARNT heterodimers and binding to exogenous response elements (XREs) on DNA, thereby enhancing drug metabolizing enzyme activity. Sudan IV can be used to study the toxicity mechanisms of industrial dyes and the effects of interactions with serum proteins (such as bovine serum albumin (BSA)) on their distribution in vivo. Sudan IV is a fat-soluble diazo dye that can be used to stain lipids, triglycerides, and lipoproteins on frozen sections.

Versicolorin A is a biosynthetic precursor of Aflatoxin B1 (HY-N6615). Versicolorin A induces phosphorylation of p53. Versicolorin A activates the aryl hydrocarbon receptor AhR and significantly induces the expression of CYP1A1. Versicolorin A exerts genotoxic and cytotoxic effects. Versicolorin A enhances the genotoxicity of aflatoxin B1 in cells by promoting CYP450-mediated bioactivation of aflatoxin B1. Versicolorin A can be used in research related to colorectal cancer and hepatocellular carcinoma.