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Results for "

CYP3A4-inhibitor

" in MedChemExpress (MCE) Product Catalog:

12

Inhibitors & Agonists

2

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0105A
    (+)-Ketoconazole

    (+)-Ketoconazol; (+)-R 41400

    		 Fungal Cytochrome P450 Infection
    (+)-Ketoconazole ((+)-R 41400) is an imidazole anti-fungal agent, a CYP3A4 inhibitor.
    (+)-Ketoconazole
  • HY-12035
    AMG-208
    1 Publications Verification

    		 c-Met/HGFR Cytochrome P450 Cancer
    AMG-208 is an orally active c-Met/RON dual selective inhibitor with an IC50 of 9 nM for c-Met. AMG-208 is a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity .
    AMG-208
  • HY-120696
    SR9186

    ML368

    		 Cytochrome P450 Parasite Infection
    SR9186 (ML368) is a potent CYP3A4 inhibitor with IC50 s for inhibition of midazolam → 1′hydroxymidazolam, testosterone → 6β-hydroxytestosterone, and vincristine → vincristine M1 of 9, 4, and 38 nM, respectively. SR-9186 inhibits liver-stage development of P. falciparum to block ivermectin metabolism .
    SR9186
  • HY-N2259
    Curcumenol
    3 Publications Verification

    (+)-Curcumenol

    		 Cytochrome P450 Neurological Disease Inflammation/Immunology Cancer
    Curcumenol ((+)-Curcumenol) is a potent CYP3A4 inhibitor with an IC50 of 12.6 μM, which is one of constituents in the plants of medicinally important genus of Curcuma zedoaria, with neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. Curcumenol ((+)-Curcumenol) suppresses Akt-mediated NF-κB activation and p38 MAPK signaling pathway in LPS-stimulated BV-2 microglial cells .
    Curcumenol
  • HY-119293
    K777
    1 Publications Verification

    		 Cathepsin CCR Cytochrome P450 Parasite SARS-CoV Filovirus Infection Cancer
    K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively .
    K777
  • HY-W740216
    N-Demethyl Mifepristone

    RU 42633

    		 Glucocorticoid Receptor Drug Metabolite Endocrinology
    N-Demethyl Mifepristone (RU 42633) is an active metabolite of Mifepristone (HY-13683). The affinities of N-Demethyl Mifepristone to the glucocorticoid receptor is 61% compared with 100% for Mifepristone .
    N-Demethyl Mifepristone
  • HY-150574
    CYP3A4-IN-1

    		Cytochrome P450 Infection
    CYP3A4-IN-1 (compound 5a) is a potent cytochrome P450 3A4 (CYP3A4) inhibitor with an IC50 value of 0.085 µM .
    CYP3A4-IN-1
  • HY-107461
    LY2623091

    		Glucocorticoid Receptor Cardiovascular Disease
    LY2623091 is a mineralocorticoid receptor antagonist for the treatment of refractory hypertension. LY2623091 exhibits CYP3A4-dependent clearance and synergistic effects with CYP3A4 inhibitors .
    LY2623091
  • HY-117010
    Kushenol K

    		Cytochrome P450 HSV SGLT Infection Metabolic Disease
    Kushenol K, a flavonoid antioxidant isolated from the roots of Sophora flavescens. Kushenol K is a cytochrome P-450 3A4 (CYP3A4) inhibitor with a Ki value of 1.35 μM . Kushenol K shows weak antiviral activity against HSV-2 (EC50 of 147 μM) . Kushenol K also inhibits the activity of SGLT1 and SGLT2 .
    Kushenol K
  • HY-119293A
    K777 tosylate

    		Cathepsin CCR Cytochrome P450 Parasite SARS-CoV Filovirus Infection Cancer
    K777 tosylate is a potent, orally active and irreversible cysteine protease inhibitor. K777 tosylate is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 tosylate irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 tosylate is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 tosylate inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively .
    K777 tosylate
  • HY-121057
    3-Hydroxyflunitrazepam

    3-OH FNTZ

    		 Drug Metabolite Cytochrome P450 Metabolic Disease
    3-Hydroxyflunitrazepam (3-OH FNTZ) is the major metabolite of Flunitrazepam (FNTZ), generated via 3-hydroxylation by CYP3A4 (Km = 286 μM), and represents the dominant metabolic pathway (>80%) in liver microsomes. Its formation is significantly inhibited by CYP3A4 inhibitors such as Ketoconazole (HY-B0105) (IC50 = 0.11 μM) and Ritonavir (HY-90001) (IC50 = 0.041 μM), indicating a strong dependence on CYP3A4 activity and potential drug interactions .
    3-Hydroxyflunitrazepam
  • HY-10672
    Urotensin-II receptor antagonist-1

    		Urotensin Receptor Cytochrome P450 Sodium Channel Opioid Receptor Cardiovascular Disease
    Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, Ki=16 nM (test on HEK293 cells expressing recombinant human UT receptor). Urotensin-II receptor antagonist-1 inhibits cytochrome P450 (IC50=0.75 μM, CYP2D6; 1.4 μM, CYP3A4), inhibits κ-opioid receptor (EC50=3.2 μM), targets cardiac sodium channels (Ki=2.5 μM) .
    Urotensin-II receptor antagonist-1

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