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-30151R
    Methoxsalen (Standard)
    Inhibitor
    Methoxsalen (Standard) is the analytical standard of Methoxsalen. This product is intended for research and analytical applications. Methoxsalen (8-Methoxypsoralen) is a furanocoumarin compound used in psoralen, used in studies of psoriasis, eczema, vitiligo and some sun-exposed cutaneous lymphomas, and is a P450 inhibitor.
    Methoxsalen (Standard)
  • HY-N3758
    Dihydrosesamin
    Dihydrosesamin is a Lignans product that can be isolated from the young shoots of Chamaecyparis obtusa cv. Breviramea..
    Dihydrosesamin
  • HY-111052R
    AZD7325 (Standard)
    Activator
    AZD7325 (Standard) is the analytical standard of AZD7325. This product is intended for research and analytical applications. AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.
    AZD7325 (Standard)
  • HY-B1812S4
    Veratrole-d2-1
    Substrate
    Veratrole-d2-1 is the deuterium labeled Veratrole (HY-B1812). Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii.
    Veratrole-d<sub>2</sub>-1
  • HY-130318
    Quinidine N-oxide
    Control
    Quinidine N-oxide is a pharmacologically inactive metabolite of Quinidine (HY-B1751H). Quinidine is an active probe of CYP3A4.
    Quinidine N-oxide
  • 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-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-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)
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