1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Cytochrome P450

Cytochrome P450

CYPs

Cytochrome p450 comprises a superfamily of heme-thiolate proteins named for the spectral absorbance peak of their carbon-monoxide-bound species at 450 nm. Having been found in every class of organism, including Archaea, the p450 superfamily is believed to have originated from an ancestral gene that existed over 3 billion years ago. Repeated gene duplications have subsequently given rise to one of the largest of multigene families. These enzymes are notable both for the diversity of reactions that they catalyze and the range of chemically dissimilar substrates upon which they act. Cytochrome p450s support the oxidative, peroxidative and reductive metabolism of such endogenous and xenobiotic substrates as environmental pollutants, agrochemicals, plant allelochemicals, steroids, prostaglandins and fatty acids. In humans, Cytochrome p450s are best known for their central role in phase I drug metabolism where they are of critical importance to two of the most significant problems in clinical pharmacology: drug interactions and interindividual variability in drug metabolism.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15996A
    Seviteronel (R enantiomer)
    98.82%
    Seviteronel R enantiomer (VT-464 R enantiomer) is the R enantiomer of Seviteronel (VT-464), which is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM); Seviteronel (VT-464) R enantiomer's activity is unknown.
    Seviteronel (R enantiomer)
  • HY-151239
    ONT-993
    Inhibitor 99.85%
    ONT-993 is an aliphatic hydroxylated metabolite. ONT-993 inhibits CYP2D6 (IC50=7.9 µM) and causes metabolism-dependent inactivation of CYP3A (KI=1.6 µM).
    ONT-993
  • HY-N6748
    Roquefortine C
    Inhibitor 98.42%
    Roquefortine C, a fungal cyclopeptide isolated from Penicillium roquefortii, activates P-gp and also inhibits P450-3A and other haemoproteins. Roquefortine C has bacteriostatic activities against Gram-positive bacteria.
    Roquefortine C
  • HY-N1282
    Seneciphylline
    Inhibitor 99.93%
    Seneciphylline is a toxic pyrrolizidine alkaloid in Gynura japonica. Seneciphylline significantly increases the activities of epoxide hydrase and glutathione-S-transferase but causes reduction of cytochrome P-450 and related monooxygenase activities.
    Seneciphylline
  • HY-101676
    RG-12525
    Inhibitor 98.31%
    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.
    RG-12525
  • HY-14248S
    Letrozole-d4
    99.82%
    Letrozole-d4 (CGS 20267-d4) is the deuterium labeled Letrozole. Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer[1][2][3].
    Letrozole-d<sub>4</sub>
  • HY-B0189B
    Mosapride citrate dihydrate
    Inducer
    Mosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with 5-hydroxytryptamine4 receptor agonist activity and has been widely used in the research of a variety of gastrointestinal disorders. Mosapride citrate dihydrate potently inhibits Kv4.3 in a concentration-dependent manner with IC50 values of 15.2 μM. Mosapride citrate dihydrateselectively stimulates upper GI motility in vivo.
    Mosapride citrate dihydrate
  • HY-B0258S
    Gemfibrozil-d6
    Inhibitor 98.00%
    Gemfibrozil-d6 is the deuterium labeled Gemfibrozil. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
    Gemfibrozil-d<sub>6</sub>
  • HY-Z0056S
    Bromobenzene-d5
    98.66%
    Bromobenzene-d5 is the deuterium labeled Bromobenzene. Bromobenzene is a well-known environmental toxin which causes liver and kidney damage through CYP450-mediated bio-activation to generate reactive metabolites and, consequently, oxidative stress[1].
    Bromobenzene-d<sub>5</sub>
  • HY-118178
    LY43578
    Inhibitor 99.76%
    LY43578 is an orally active aromatase inhibitor. LY43578 inhibits P-450-dependent p-nitroanisole O-demethylation and ethylmorphine N-demethylation in hepatic microsomes isolated from rat, with the IC50 of 0.3 and 5 μΜ, respectively. LY43578 can be used for neurological disorder study.
    LY43578
  • HY-113986
    Dexfadrostat
    Inhibitor 98.75%
    Dexfadrostat ((R)-Fadrozole) is a potent nonsteroidal inhibitor. Dexfadrostat also inhibits human placental aromatase (pIC50 = 6.17) and aldosterone biosynthesis. Dexfadrostat reverses cardiac fibrosis in spontaneously hypertensive heart failure rats..
    Dexfadrostat
  • HY-17514S
    Itraconazole-d5
    Inhibitor 99.55%
    Itraconazole-d5 is the deuterium labeled Itraconazole. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects[1][2][3].
    Itraconazole-d<sub>5</sub>
  • HY-N0893R
    Tetrahydrocurcumin (Standard)
    Inhibitor
    Tetrahydrocurcumin (Standard) is the analytical standard of Tetrahydrocurcumin. This product is intended for research and analytical applications. Tetrahydrocurcumin is a Curcuminoid found in turmeric (Curcuma longa) that is produced by the reduction of Curcumin. Tetrahydrocurcumin inhibit CYP2C9 and CYP3A4.
    Tetrahydrocurcumin (Standard)
  • HY-155002
    hCYP3A4 Fluorogenic substrate 1
    99.27%
    hCYP3A4 Fluorogenic substrate 1 is a potrnt hCYP3A4 fluorogenic substrate with an Km value of 0.36 μM. hCYP3A4 Fluorogenic substrate 1 can be used for cell and in vivo imaging.
    hCYP3A4 Fluorogenic substrate 1
  • HY-100331
    MCH-1 antagonist 1
    Inhibitor
    MCH-1 antagonist 1 is a potent melanin concentrating hormone (MCH-1) antagonist with a Ki of 2.6 nM. MCH-1 antagonist 1 also inhibits CYP3A4 with an IC50 of 10 μM.
    MCH-1 antagonist 1
  • HY-N8382
    Chalepensin
    Inhibitor ≥98.0%
    Chalepensin, a furanocoumarin, is a competitive CYP2A6 inhibitor. Chalepensin also inhibits human CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to different extents.
    Chalepensin
  • HY-122277
    1'-Hydroxy bufuralol
    1'-Hydroxy bufuralol, the main metabolite of bufuralol, can reflect CYP2D activity.
    1'-Hydroxy bufuralol
  • HY-N9551
    Eriodictyol chalcone
    Inhibitor
    Eriodictyol chalcone possesses both anti-aromatase and an anti-17β-HSD activity.
    Eriodictyol chalcone
  • HY-100902
    CDD3506
    Activator 98.03%
    CDD3506 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
    CDD3506
  • HY-B0105S1
    Ketoconazole-d4
    Inhibitor ≥98.0%
    Ketoconazole-d4 is the deuterium labeled Ketoconazole. Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.
    Ketoconazole-d<sub>4</sub>
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