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-19379
    E-2101
    Inhibitor
    E-2101 is a novel antispastic agent. E-2101 is a competitive CYP2C19 and CYP2D6 inhibitor with Ki values of 15 and 48 μM, respectively. E-2101 is metabolized by Cytochromes P450 to form monohydroxylated (M1 and M2), dihydroxylated (M3), and N-dealkylated metabolites (M4). E-2101 can be used in the research of skeletal muscle spasm.
    E-2101
  • HY-B1462S2
    Chlorzoxazone-13C,15N,d2
    Modulator
    Chlorzoxazone-13C,15N,d2 is 13C-, 15N-, and deuterium-labeled Chlorzoxazone (HY-B1462).
    Chlorzoxazone-<sup>13</sup>C,<sup>15</sup>N,d<sub>2</sub>
  • HY-123247
    LY113174
    Inhibitor
    LY113174 is an orally active aromatase inhibitor (IC50 = 24 nM). LY113174 blocks testosterone induced increase in uterine weight in rat, and inhibits ovarian estrogen biosynthesis.
    LY113174
  • HY-B0258S1
    Gemfibrozil-d6-1
    Inhibitor
    Gemfibrozil-d6-1 (CI-719-d6-1) is the deuterium labeled Gemfibrozil (HY-B0258). 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>-1
  • HY-N1407R
    Polygalaxanthone III (Standard)
    Inhibitor
    Polygalaxanthone III (Standard) is the analytical standard of Polygalaxanthone III. This product is intended for research and analytical applications. Polygalaxanthone III is extracted from polygala tenuifolia wild, has inhibitory effect towards CYP450 enzyme. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC50 of 50.56 μM.
    Polygalaxanthone III (Standard)
  • HY-119209R
    Nefazodone (Standard)
    Inhibitor
    Nefazodone (Standard) is the analytical standard of Nefazodone. This product is intended for research and analytical applications. Nefazodone is an orally active phenylpiperazine antidepressant. Nefazodone can potently and selectively block postsynaptic 5-HT2A receptors, and moderately inhibit 5-HT and noradrenaline reuptake. Nefazodone can also relieve the adverse effects of stress on the the immune system of mice. Nefazodone has a high affinity for CYP3A4 isoenzyme, which indicates that it has certain risk of agent-agent interaction.
    Nefazodone (Standard)
  • HY-113907
    SDZ-285604
    Inhibitor
    SDZ-285604 (VNF) is a T. cruzi CYP51 inhibitor and can be used for study of Trypanosoma cruzi infection.
    SDZ-285604
  • HY-125833R
    Alpha-Naphthoflavone (Standard)
    Inhibitor
    Alpha-Naphthoflavone (Standard) is the analytical standard of Alpha-Naphthoflavone. This product is intended for research and analytical applications. Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis.
    Alpha-Naphthoflavone (Standard)
  • HY-174394S
    CYP51-IN-25
    Inhibitor
    CYP51-IN-25 is a orally active broad spectrum antifungal agent with the MIC80 of 0.00625-0.05 μg/mL. is a CYP51-IN-25 is a deuterated compound with antibiotic properties. CYP51-IN-25 can inhibit the fungal CYP51 enzyme, block ergosterol synthesis, and disrupt cell membrane integrity. CYP51-IN-25 can be used for research on fungal infections.
    CYP51-IN-25
  • HY-116034
    Arasertaconazole
    Inhibitor
    Arasertaconazole is a potent 14α-lanosterol demethylase inhibitor. Arasertaconazole has antifungal and antibacterial activity.
    Arasertaconazole
  • HY-13463AR
    Avatrombopag maleate (Standard)
    Activator
    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.
    Avatrombopag maleate (Standard)
  • HY-138051
    TUPS
    Inhibitor
    TUPS can inhibit the gene expression of epoxide hydrolase (sEH) and cytochrome P450 (CYP). TUPS can be used in cardiovascular disease-related research.
    TUPS
  • HY-14275R
    Verapamil (Standard)
    Inhibitor
    Verapamil (Standard) is the analytical standard of Verapamil. This product is intended for research and analytical applications. Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research.
    Verapamil (Standard)
  • HY-N0494R
    Gentiopicroside (Standard)
    Inhibitor
    Gentiopicroside (Standard) is the analytical standard of Gentiopicroside. This product is intended for research and analytical applications. Gentiopicroside, a naturally occurring iridoid glycoside, inhibits P450 activity, with an IC50 and a Ki of 61 μM and 22.8 μM for CYP2A6; Gentiopicroside has anti-inflammatoryand antioxidative effects.
    Gentiopicroside (Standard)
  • HY-169217
    CYP3A4-IN-4
    Inhibitor
    CYP3A4-IN-4 (compound Δ,Λ-3), a Ru(II)−Ir(III) Conjugate, is a photoactive inhibitor of the major human drug metabolizing enzyme CYP3A4. CYP3A4-IN-4 containing the [Ru(tpy)(Me2bpy)] photocaging group showed an IC50 of 2.2 μM for inhibition of microsomal CYP3A4 under light conditions (λirr=530 nm, tirr=15 min). CYP3A4-IN-4 shows the phototherapeutic index (PI) for of 5.4.
    CYP3A4-IN-4
  • HY-129105R
    Clomethiazole (Standard)
    Inhibitor
    Clomethiazole (Standard) is the analytical standard of Clomethiazole. This product is intended for research and analytical applications. Chlormethiazole is an potent and orally active GABAA agonist. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus.
    Clomethiazole (Standard)
  • HY-159741
    Minamestane
    Inhibitor
    Minamestane (FCE 24928) is a selective and competitive aromatase inhibitor with an IC50 value of 45.7 nM. Minamestane is promising for research of postmenopausal breast cancer.
    Minamestane
  • HY-109040R
    Quilseconazole (Standard)
    Inhibitor
    Quilseconazole (Standard) is the analytical standard of Quilseconazole (HY-109040). This product is intended for research and analytical applications. Quilseconazole (VT-1129) is an orally active, highly selective fungal cytochrome P450 enzyme Cyp51 inhibitor that can cross the blood-brain barrier. Quilseconazole prevents the synthesis of ergosterol, an important component of the fungal cell membrane, by inhibiting Cyp51. Quilseconazole has minimal effects on human CYP enzymes. Quilseconazole has antifungal activity and can be used in the study of cryptococcal meningitis and other diseases.
    Quilseconazole (Standard)
  • HY-116686
    Inz-1
    Inhibitor
    Inz-1 is a potent and selective mitochondrial cytochrome bc1 inhibitor for yeast (IC50=8.092 μM) over humans (IC50=45.320 μM). Inz-1 reverses Fluconazole (HY-B0101) or other triazole antifungals’ resistance in the pathogenic fungus Candida albicans.
    Inz-1
  • HY-N2625AR
    Harmalol hydrochloride (Standard)
    Harmalol (hydrochloride) (Standard) is the analytical standard of Harmalol (hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity

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