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-157959
    Orphenadrine
    Inducer 99.11%
    Orphenadrine ((±)-Orphenadrine) is a skeletal muscle relaxant and NMDA antagonist that also has antiparkinsonian, antihistamine, antitremor, antispasmodic, and analgesic effects. Orphenadrine inhibits the binding of [3H]MK-801 to the phencyclidine (PCP) binding site of the NMDA receptor. Orphenadrine is also an anticholinergic and cytochrome P450 (CYP) 2B inducer. Orphenadrine may exert pro-tumor effects, causing CAR nuclear translocation, resulting in microsomal reactive oxygen species (ROS) production and oxidative stress. Orphenadrine also exerts neuronal protection, protecting rat cerebellar granule cells (CGC) from 3-NPA-induced death and has inhibitory potential against neurodegenerative diseases mediated by NMDA receptor overactivation.
    Orphenadrine
  • 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-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 an orally effective hepatotoxic inducer. Seneciphylline is metabolized by CYP450 enzymes into active intermediates, which covalently bind to intracellular biomacromolecules such as proteins and DNA to form adducts, which in turn trigger a series of toxic reactions, such as inducing cell apoptosis and damaging mitochondrial function. Seneciphylline can be used in hepatotoxicity research[1][2].
    Seneciphylline
  • HY-W000343
    1-Tritylimidazole
    Inducer 99.06%
    1-Tritylimidazole is an inducer of cytochrome P450 (Cytochrome P450).
    1-Tritylimidazole
  • 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-145786
    Abiraterone decanoate
    Inhibitor 99.69%
    Abiraterone decanoate is a potent Abiraterone proagent. Abiraterone decanoate provide a controlled release of Abiraterone and long-acting CYP17 inhibition with intramuscular (IM) delivery.
    Abiraterone decanoate
  • HY-12433
    BMS-819881
    Inhibitor
    BMS-819881 is a melaninconcentrating hormone receptor 1 (MCHR1) antagonist, which binds rat MCHR1 with a Ki of 7 nM. BMS-819881 also is selective and potent for CYP3A4 activity with an EC50 of 13 μM.
    BMS-819881
  • 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-B1462S
    Chlorzoxazone-d3
    Modulator 98.50%
    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.
    Chlorzoxazone-d<sub>3</sub>
  • HY-N12257
    Antimycin A2
    Inhibitor 98.02%
    Antimycin A2 is the component of the antibiotic antimycin A. Antimycin A is an antibiotic, that exhibits inhibitory activity against fungi and some insects through inhibition of respiration and cytochrome b reoxidation.
    Antimycin A2
  • 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-127112
    Oleic acid alkyne
    99.96%
    Oleic acid alkyne is oleic acid with an acetylene group. The terminal alkyne group can be used for click chemical ligation reactions. Oleic acid can be hydroxylated by a microsomal cytochrome P-450-dependent system (ω-OAH). Through click chemistry reactions, fluorescent or biotin-labeled oleic acid can be introduced to analyze its metabolism and biological activity.
    Oleic acid alkyne
  • 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
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