2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Cytochrome P450
  5. CYP1A2 Isoform

CYP1A2

CYP1A2 is a major hepatic cytochrome P450 enzyme that contributes approximately 5-20% of the total microsomal P450 pool and catalyzes oxidative biotransformation of numerous clinically relevant xenobiotics and therapeutic compounds, including caffeine, clozapine, duloxetine, and theophylline[1][2]. Mechanistically, CYP1A2 functions within the phase I xenobiotic metabolism pathway, where it mediates oxidation reactions and participates in the metabolic activation of aromatic heterocyclic amines and polycyclic aromatic hydrocarbons that are associated with carcinogenic processes[1][3]. CYP1A2 expression is strongly regulated by the aryl hydrocarbon receptor (AHR) signaling network and is influenced by environmental, genetic, and inflammatory factors that contribute to substantial interindividual variability in enzyme activity[1][4]. In disease-related contexts, hepatic CYP1A2 expression is reduced during inflammation, cholestasis, and sepsis, linking altered CYP1A2 activity to pathological changes in drug metabolism and toxicological responses[1][5]. Compared with related family members, CYP1A2 is constitutively expressed in the liver, whereas CYP1A1 shows broader inducible expression patterns despite substantial substrate overlap, making isoform-specific characterization essential for accurate drug metabolism studies[3][6]. For experimental applications, selective inhibition approaches and humanized mouse models have been used to distinguish CYP1A2-mediated metabolism from CYP1A1 activity and to improve prediction of xenobiotic disposition and pharmacokinetic outcomes[3].

CYP1A2 Related Products (5):

Cat. No. Product Name Effect Purity
  • HY-120717
    VU6001966
    		Inhibitor 99.89%
    VU6001966 is a brain-penetrant and selective mGlu2 receptor inhibitor. VU6001966 blocks mGlu2 receptor activity, counteracts LY379268 (HY-103558)-mediated blood-brain barrier protection and inflammatory cytokine dampening in microglia under inflammatory conditions. VU6001966 enhances antidepressant effects when combined with Scopolamine (HY-N0296). VU6001966 can be used for the research of major depressive disorder.
  • HY-132845
    Utreloxastat
    		Inhibitor 99.32%
    Utreloxastat (PTC857) is an orally active and blood-brain barrier-permeable 15-lipooxygenase inhibitor. Utreloxastat is a weak inhibitor of CYP1A2 and 2B6 with an IC50 of >5.3 μM. Utreloxastat reduces oxidative stress and inhibits the consumption of reduced glutathione and ferroptosis. Utreloxastat can be used in the study of neurodegenerative diseases characterized by high levels of oxidative stress and mitochondrial pathology, such as amyotrophic lateral sclerosisc.
  • HY-170846
    FGFRs-IN-1
    		Inhibitor
    FGFRs-IN-1 (Compound A16) is the orally active inhibitor for FGFR, that inhibits FGFR1/2/3/4 with IC50s of 2.3, 7, 11, and 163 nM, respectively. FGFRs-IN-1 also inhibits VEGFR1/2/3, Abl, and Flt3 with IC50s of 61, 176, 112, 26, and 353 nM, respectively. FGFRs-IN-1 exhibits weak inhibitory efficacy against CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF-β1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model.
  • HY-19397
    BMS-223131
    		Inhibitor
    BMS-223131 (Compound 1) is a potent maxi-K potassium channel opener. BMS-223131 has a strong inhibitory effect on the CYP2C9 enzyme (IC50 = 1.7 μM) and also shows varying degrees of inhibition on other common CYP enzymes such as CYP1A2, CYP2C19, CYP2D6, and CYP3A4. BMS-223131 can enhance the outward current mediated by maxi-K, by promoting K+ efflux to hyperpolarize the cell membrane and reducing Ca2+ influx. BMS-223131 can be used for the research of neurological disease, such as stroke.
  • HY-174417
    NNRT-IN-10
    		Inhibitor
    NNRT-IN-10 is a potent, selective and orally active non-nucleoside HIV-1 reverse transcriptase (NNRTI) inhibitor with with an EC50 values ranging from 1.16 to 18.3 nM for HIV and its mutant strains. NNRT-IN-10 exhibits good pharmacokinetic properties and favorable safety profiles. NNRT-IN-10 can be used for the study of AIDS, caused by HIV-1.