2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Cytochrome P450
  5. CYP3A4 Isoform
  6. CYP3A4 Inhibitor

CYP3A4 Inhibitor

CYP3A4 Inhibitors (9):

Cat. No. Product Name Effect Purity
  • 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.
  • HY-N0926A
    Columbamine chloride
    		Inhibitor 99.62%
    Columbamine (Columbamin; Dehydroisocorypalmine) chloride is an organic heterotetracyclic alkaloid extracted from plants. Columbamine chloride is a metabolite of Berberine (HY-N0716). Columbamine chloride inhibits the cytochrome P450 (CYP) isoform CYP3A4 (IC50 = 30.6 µM). Columbamine chloride induces apoptosis in cancer cells. Columbamine chloride can be used for antioxidant, anti-inflammatory, antitumor, antifungal, antiparasite, hepatoprotective, neuroprotective, hypolipidemic and hypoglycemic study.
  • HY-P10032A
    NN1177 TFA
    		Inhibitor 98.66%
    NN1177 (NNC9204-1177) TFA is a long-acting GLP-1/glucagon receptor co-agonist. NN1177 TFA can induce a dose-dependent body weight loss in diet-induced obese (DIO) mice.
  • HY-N0926
    Columbamine
    		Inhibitor 99.70%
    Columbamine (Columbamin; Dehydroisocorypalmine) is an organic heterotetracyclic alkaloid extracted from plants. Columbamine is a metabolite of Berberine (HY-N0716). Columbamine inhibits the cytochrome P450 (CYP) isoform CYP3A4 (IC50 = 30.6 µM). Columbamine induces apoptosis in cancer cells. Columbamine can be used for antioxidant, anti-inflammatory, antitumor, antifungal, antiparasite, hepatoprotective, neuroprotective, hypolipidemic and hypoglycemic study.
  • HY-133798
    Sorafenib N-oxide
    		Inhibitor
    Sorafenib N-oxide is an active metabolite of sorafenib (HY-10201). Sorafenib N-oxide is a linear-mixed inhibitor of microsomal CYP3A4, with a Ki of 15 μM.
  • 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-10779
    BMS-344577
    		Inhibitor
    BMS-344577 (Compound 22) is a potent and orally active factor Xa inhibitor (IC50 = 4 nM, EC2xPT = 7 μM). BMS-344577 shows potent CYP3A4 inhibition activity (IC50 = 0.3 μM). BMS-344577 can be used for the research of cardiovascular disease.
  • HY-158435
    P-gp inhibitor 23
    		Inhibitor
    P-gp inhibitor 23 (compound 14F) is a potent inhibitor of P-gp and CYP3A4, with the EC50 and IC50 of 28 nM and 223 nM, respectively.
  • HY-10575
    MK-5596
    		Inhibitor
    MK-5596 is an efficient, selective and orally active CB1R (IC50 = 1.0 nM, EC50 = 5.8 nM) inverse agonist. MK-5596 has weak hERG inhibitory activity. MK-5596 has strong weight loss and appetite suppression effects. MK-5596 has a certain inhibitory effect on CYP enzymes (CYP3A4: IC50 = 3.3 μM, CYP2C8: IC50 = 11 μM, CYP2C9: IC50 = 18 μM, CYP2D6: IC50 = 6 μM). MK-5596 can be used for research on conditions such as obesity.