Cytochrome P450 Inhibitor

(E/Z)-DMU2139 (Compound 180) is the E/Z isomer of DMU2139 (HY-101285). (E/Z)-DMU2139 is a potent and specific CYP1B1 inhibitor (IC₅₀: 4 nM).

Aminoglutethimide phosphate (DL-Aminoglutethimide phosphate) is an orally active anticonvulsant with various endocrine-related side effects. Aminoglutethimide phosphate blocks multiple steroid hormone synthesis pathways by inhibiting several cytochrome P-450-dependent hydroxylases, such as aromatase, cholesterol side-chain cleavage enzyme, 11-hydroxylase, and 18-hydroxylase, with IC₅₀ values of 0.3, 3.5, 120, and 20 μM, respectively. Aminoglutethimide phosphate reduces cortisol levels. Aminoglutethimide phosphate can be used in research on Cushing's syndrome, breast cancer, and other conditions.

(+)-Menthofuran (compound 1) is a furan terpenoid that can be found in mint oils.

Olivetol (Standard) is the analytical standard of Olivetol. This product is intended for research and analytical applications. Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively.

8-Hydroxywarfarin (8-OH Warfarin) is a CYP2C9 inhibitor. 8-Hydroxywarfarin inactivates the anticoagulant activity of Warfarin (HY-B0687) via 8-hydroxylation. 8-Hydroxywarfarin serves as a glucuronidation substrate for UGT1A1, UGT1A8, UGT1A9, as well as wild-type/mutant UGT1A10. This reaction enhances its polarity, solubility and excretion efficiency, and the process is independent of phenylalanine⁹⁰ of UGT1A10. 8-Hydroxywarfarin can be used in studies related to thromboembolic diseases.

CYP450-IN-1 (compound 2e) is a potent inhibitor of CYP450.

Becliconazole is a fungal CYP51A1 inhibitor. Becliconazole can be used in research on fungal infections.

Fadrozole (hydrochloride) (Standard) is the analytical standard of Fadrozole (hydrochloride). This product is intended for research and analytical applications. Fadrozole hydrochloride (CGS 16949A) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.

CYP51-IN-27 is a sterol 14α-demethylase CYP51 inhibitor with an IC₅₀ of 0.3434 μg/mL. CYP51-IN-27 exhibits antifungal activity and inhibits the production of fungal ergosterol. CYP51-IN-27 can be used for the research of infection, such as rice sheath blight.

APD668 (Standard) is the analytical standard of APD668. This product is intended for research and analytical applications. APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes.

RG-12525 (Standard) is the analytical standard of RG-12525 (HY-101676). This product is intended for research and analytical applications. RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 μM.

Atovaquone (Standard) is the analytical standard of Atovaquone. This product is intended for research and analytical applications. Atovaquone (Atavaquone) is a potent, selective and orally active inhibitor of the parasite’s mitochondrial cytochrome bc1 complex. Atovaquone is against human and  P. falciparum cytochrome bc1 activity with IC₅₀ values of 460 nM and 2.0 nM, respectively. Atovaquone is an antimalarial agent and has the potential for the investigation of neumocystis pneumonia, toxoplasmosis, malaria, and babesia.

Octinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo.

Antifungal agent 114 (Compound 19g) is an inhibitor for Cytochrome P450, that inhibits CYP1A2, CYP2C9, CYP2C19 CYP2D6 and CYP3A4 at 10 μM. Antifungal agent 114 exhibits antifungal activity against Cryptococcus neoformans, Candida and Aspergillus, with MIC <0.0625 μg/mL. Antifungal agent 114 exhibits good metabolic stability in human liver microsomes with a half-time of 107 minutes.

meso-Zeaxanthin ((3R,3′S)-Zeaxanthin) is an orally active xanthophyll carotenoid. meso-Zeaxanthin inhibits CYP1A1, CYP1A2, CYP2B1/2, COX-2, TNF-α and iNOS, and enhances the activities of Uridine diphosphate glucuronosyltransferase and Glutathione-S-transferase. meso-Zeaxanthin quenches oxygen free radicals. meso-Zeaxanthin filters short-wavelength blue light, alleviates oxidative damage and visual abnormalities. meso-Zeaxanthin reduces tumor incidence, prolongs tumor latency and survival rate of tumor-bearing mice, and inhibits paw edema. meso-Zeaxanthin can be used in research related to sarcoma and age-related macular degeneration.

Sulfamethylphenazole sodium (Sulfapyrazole sodium; Vesulong sodium) is a long-acting sulfonamide antibacterial agent. Sulfamethylphenazole sodium maintains effective chemotherapeutic blood concentrations through the slow release of free sulfonamide from a protein-binding reservoir and can be used in combination with antibiotics such as Terramycin for bovine hemorrhagic septicemia. Sulfamethylphenazole sodium exhibits moderate antimycobacterial activity against Mycobacterium tuberculosis H37Rv (MIC = 15.38 μg/mL) and inhibitory activity against CYP 2C9. Sulfamethylphenazole sodium can be used in studies related to tuberculosis and hemorrhagic septicemia.

Dibenzothiophene (Standard) is the analytical standard of Dibenzothiophene (HY-B0973). This product is intended for research and analytical applications. Dibenzothiophene is an orally active and a noncompetitive CYP1A inhibitor. Dibenzothiophene inhibits CYP1A-mediated EROD activity with K_m of 0.592 μM. Dibenzothiophene interacts with the AHR pathway. Dibenzothiophene enhances the embryotoxicity of β-naphthoflavone (HY-114740). Dibenzothiophene shows acute toxicity in mice. Dibenzothiophene is mainly used for the study of the mechanism of developmental toxicity in organisms.

CYP51-IN-10 is cytochrome P450 14a-demethylase (CYP51) inhibitor with antifungal activity. CYP51-IN-10 can be used for the research of fungal infection.

3'-Methoxy-4'-nitroflavone (MNF) is a specific aryl hydrocarbon receptor (AhR) antagonist. 3'-Methoxy-4'-nitroflavone activates AhR by inhibiting CYP1, the metabolic enzyme of the endogenous ligand FICZ (HY-12451), leading to the accumulation of FICZ. 3'-Methoxy-4'-nitroflavone reverses the anti-apoptotic effect of TCDD, attenuates the activation of Akt and Erk1/2 kinases and the expression of TGFα induced by TCDD. 3'-Methoxy-4'-nitroflavone can be used in research related to breast tumor promotion, rheumatoid arthritis, multiple sclerosis and inflammatory bowel disease.

SKF 104976 is a 3,2-carboxylic acid derivative with potent 14-alpha-demethylase (14 alpha DM) inhibitory activity. SKF 104976 inhibited 14 alpha DM activity by 50% at 2 nM in Hep G2 cell extracts. SKF 104976 inhibited the incorporation of [14C]acetate into cholesterol in intact cells at similar concentrations, accompanied by accumulation of lanosterol, and resulted in a 40-70% decrease in 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) activity. SKF 104976 did not affect the uptake and degradation of low-density lipoprotein in Hep G2 cells, indicating that HMGR and low-density lipoprotein receptor activities are not coordinately regulated under these conditions. The inhibitory effect of SKF 104976 on HMGR activity remained unchanged even when the flux of carbon units in the sterol synthesis pathway was reduced by 80%. SKF 104976 did not inhibit HMGR activity under conditions where sterol synthesis was almost completely blocked by lovastatin.