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-W267897
    7-Benzyloxy-4-(trifluoromethyl)coumarin
    99.47%
    7-Benzyloxy-4-(trifluoromethyl)coumarin (7-BFC) is a coumarin fluorescent substrate. 7-Benzyloxy-4-(trifluoromethyl)coumarin is a substrate for cDNA-expressed CYP1A2 and CYP3A4 and is metabolized to 7-hydroxy-4-trifluoromethylcoumarin (HFC). 7-Benzyloxy-4-(trifluoromethyl)coumarin is used for rapid CYP isoform metabolism and inhibition screening studies.
    7-Benzyloxy-4-(trifluoromethyl)coumarin
  • HY-15565
    APD668
    Inhibitor 99.73%
    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.
    APD668
  • HY-17508S
    Clarithromycin-13C,d3
    99.9%
    Clarithromycin-13C,d3 is the deuterium and 13C labeled Clarithromycin.
    Clarithromycin-<sup>13</sup>C,d<sub>3</sub>
  • HY-135560
    Nicotelline
    Inhibitor 98.88%
    Nicotelline (Nicotellin) is a nicotine-related alkaloid, as well as a weak inhibitor of human cDNA-expressed cytochrome P-450 2A6 (CYP2A6). CYP2A6 mediates coumarin 7-hydroxylation, while Nicotelline fails to exhibit inhibition at 300 μM. Nicotelline can be used as a tracer and biomarker of particulate matter (PM) derived from tobacco smoke.
    Nicotelline
  • HY-156757
    MDL-811
    Inhibitor 99.68%
    MDL-811 is a selective allosteric activator of SIRT6 with an EC50 of 5.7 μM. MDL-811 possesses anti-inflammatory, antitumor, and neuroprotective activities. MDL-811 can be used for the research of diseases such as colorectal cancer and ischemic stroke.
    MDL-811
  • HY-N5092
    7-Methylcoumarin
    99.93%
    7-Methylcoumarin is a coumarin derivative with potent hepatoprotective and antioxidant properties. 7-Methylcoumarin is a mechanism-based inhibitor for CYP2A6. 7-Methylcoumarin significantly decreases alanine aminotransferase (ALT), aspartate aminotransferase (AST), and serum bilirubin (TB) in rats with CCl4-induced liver damage, whilst restoring total protein (TP) and albumin (TA) levels in serum as well as preventing oxidative stress. 7-Methylcoumarin can decline mitotic activity of A. sativum promeristem.
    7-Methylcoumarin
  • HY-N4110
    Friedelin
    Inhibitor 99.0%
    Friedelin is derived from the leaves of Maytenus ilicifolia (Mart). Friedelin is an orally active non-competitive inhibitor of CYP3A4, with IC50 and Ki values of 10.79 μM and 6.16 μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1, with IC50 and Ki values of 22.54 μM and 18.02 μM, respectively. Friedelin can be used in research related to inflammation, neurological diseases, and metabolic disorders.
    Friedelin
  • HY-N7781
    (-)-(E)-Guggulsterone
    Agonist 99.19%
    (-)-(E)-Guggulsterone ((E)-Guggulsterone) is an orally active natural stereoisomer of Guggulsterone (HY-107738). (-)-(E)-Guggulsterone is an antagonist for the Farnesoid X Receptor (FXR) with an IC50 of 24.06 μM and possesses potent hypolipidemic properties. (-)-(E)-Guggulsterone suppresses dengue virus (DENV) replication by upregulating antiviral interferon responses by inducing HO-1 expression via Nrf2 activation. (-)-(E)-Guggulsterone exhibits antibacterial activities against Bacillus subtilis, Staphylococcus aureus and Pseudomonas aeruginosa. (-)-(E)-Guggulsterone has cardiac protective and antioxidant activities in rats.
    (-)-(E)-Guggulsterone
  • HY-135549
    Fluxapyroxad
    Inhibitor 99.96%
    Fluxapyroxad is a synthetic broad-spectrum fungicide for the control of fungal diseases. Fluxapyroxad inhibits succinate dehydrogenase in complex II of the mitochondrial respiratory chain, resulting in inhibition of spore germination, germ tubes and mycelia growth within the fungus target species.
    Fluxapyroxad
  • HY-10505
    Orteronel
    Inhibitor 99.90%
    Orteronel (TAK-700) is a highly selective inhibitor of human 17,20-lyase (CYP17) with IC50 of 38 nM, and exhibits >1000-fold selectivity over other CYPs such as 11-hydroxylase and CYP3A4.
    Orteronel
  • HY-117766
    Opelconazole
    Inhibitor 98.41%
    Opelconazole (PC945), a potent, long-acting antifungal triazole, possesses activity against a broad range of both azole-susceptible and azole-resistant strains of Aspergillus fumigatus. Opelconazole is also a potent, tightly binding inhibitor of A. fumigatus sterol 14α-demethylase activity, CYP51A and CYP51B, with IC50s of 0.23 μM and 0.22 μM, respectively.
    Opelconazole
  • HY-70013S
    Abiraterone-d4
    Inhibitor 99.48%
    Abiraterone-d4 is the deuterium labeled Abiraterone. Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
    Abiraterone-d<sub>4</sub>
  • HY-122410
    Dihydrolanosterol
    99.72%
    Dihydrolanosterol is a subtrate of CYP51 and a cholesterol biosynthesis inhibitor..
    Dihydrolanosterol
  • HY-90010
    Tolterodine tartrate
    Substrate 98.64%
    Tolterodine tartrate (Kabi-2234) is a mAChR inhibitor and substrate for cytochrome P450 enzymes. Tolterodine tartrate competitively binds acetylcholine, reduces sympathetic excitation, and inhibits involuntary bladder muscle contraction. Tolterodine tartrate restores the Nrf2/NF-κB signaling pathway, mediates protection against inflammatory response and ferroptosis. Tolterodine tartrate ameliorates LPS (HY-D1056)-induced reactive oxygen species production and lipid oxidation. Tolterodine tartrate can be used for the research of urinary tract infections and overactive bladder.
    Tolterodine tartrate
  • HY-N0598
    Ginsenoside F1
    Inhibitor 99.86%
    Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.
    Ginsenoside F1
  • HY-N0920
    Dihydrokavain
    Inhibitor 99.94%
    Dihydrokavain (7,8-Dihydrokawain) is a natural kavalactone compound. Dihydrokavain inhibits COX-1, COX-2, CYP2C9 (IC50 = 130.95 μM), CYP2C19 (IC50 = 10.05 μM) and CYP3A4 (IC50 = 78.59 μM). Dihydrokavain reduces TNFα secretion. Dihydrokavain shows analgesic and anxiolytic effects.
    Dihydrokavain
  • HY-N0911
    Rehmannioside A
    Inhibitor 99.96%
    Rehmannioside A is a compound that can be isolated from Rehmanniae radix. Rehmannioside A is an inhibitor of CYP3A4, 2C9 and 2D6, with IC50 values of 10.08, 12.62 and 16.43 μM, respectively. Rehmannioside A has anti-inflammatory, antioxidant, anti-apoptosis, anti-ferroptosis, cognitive improvement and neuroprotective activities. Rehmannioside A can be used for the research of nervous system and inflammation-related diseases.
    Rehmannioside A
  • HY-W006230
    Anthraflavic acid
    Inhibitor 99.51%
    Anthraflavic acid specifically inhibits the activity of cytochrome P-448 without affecting phenobarbital-induced cytochrome P-450 or NADPH-dependent cytochrome c reduction. Anthraflavic acid inhibits cytosolic metabolic pathways, blocks the microsomal and cytosolic activation of IQ, and reduces the metabolic activation level of Glu-P-I. Anthraflavic acid may exert anticancer activity by inhibiting the metabolic activation of chemical carcinogens. Anthraflavic acid is applicable to cancer-related research.
    Anthraflavic acid
  • HY-N2625A
    Harmalol hydrochloride
    99.91%
    Harmalol hydrochloride, a beta carboline alkaloid, presents in several medicinal plants such as Peganum harmala. Harmalol hydrochloride, main metabolite of Harmaline, significantly inhibits the dioxin-mediated induction of CYP1A1 at the transcriptional and posttranslational levels. Harmalol hydrochloride possesses antioxidant and hydroxyl radical-scavenging properties.
    Harmalol hydrochloride
  • HY-133668
    Monoethyl phthalate
    Activator 98.58%
    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.
    Monoethyl phthalate
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