Catalog No.
Product Name
Application
Product Information
Citations
- Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina) is an orally active inhibitor of platelet aggregation induced by adenosine diphosphate (ADP).
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anti-inflammatory agent
Cepharanthine is an alkaloid derived from Stephania cepharantha Hayata, with possesses anti-inflammatory and antioxidative activities. -
CYP3A4 inducer
RO6889678 is an inhibitor of HBV with a complex ADME profile. RO6889678 showed an intracellular enrichment of 78-fold in hepatocytes, with an apparent intrinsic clearance of 5.2 ?l/min per mg protein and uptake and biliary clearances of 2.6 and 1.6 ?l/min per mg protein, respectively. -
Cholesterol 24-hydroxylase (CH24H) inhibitor
Soticlestat, also known as TAK 935 and OV935, is an inhibitor of the enzyme cholesterol 24-hydroxylase (CH24H). -
CYP51 inhibitor
Oteseconazole (VT-1161) is an orally active anti-fungal agent, potently binds to and inhibits Candida albicans CYP51 (Kd, <39 nM), shows no obvious effect on human CYP51. -
DAF-9 cytochrome P450 inhibitor
Dafadine-A, an analog of dafadine, is a novel inhibitor of DAF-9 cytochrome P450 in the nematode Caenorhabditis elegans; also inhibits the mammalian ortholog of DAF-9(CYP27A1). -
CYP17 lyase inhibitor
Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition. -
CYP26 inhibitor/RAMBA
Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively. -
peptidoleukotrienes antagonist
RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 ?M. -
cytochrome P450 1B1 inhibitor
1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 1B1. -
EMT inhibitor
EMT inhibitor-2 inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively. -
fungal Cyp51 inhibitor
Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes. - Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).
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Cytochrome P450 inhibitor
4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC50 of 19 nM for human P450 1B1-dependent EROD. -
CYP3A4 Inhibitor
Azithromycin, derived from erythromycin, is a antibiotic. Azithromycin binds to the 50S subunit of the bacterial ribosome, and thus inhibits translation of mRNA. -
CYP2C19/CYP2B6 inhibitor
Choline Fenofibrate (ABT-335) is the choline salt of fenofibric acid under clinical development as a combination therapy with rosuvastatin for the management of dyslipidemia. -
CYP2C9/CYP3A4 Inhibitor
Tetrahydrocurcumin-d6 is a deuterated analog of Tetrahydrocurcumin, functioning as an inhibitor of CYP2C9 and CYP3A4 enzymes. This compound exhibits significant biological activity against these cytochrome P450 isoforms, making it valuable for research into drug metabolism and pharmacokinetics. Tetrahydrocurcumin-d6 is utilized in studies aiming to elucidate the metabolic pathways and interactions of curcuminoids, as well as their potential therapeutic applications. -
CYP2C8 Inhibitor
Gemfibrozil 1-O-β-glucuronide is a competitive inhibitor of the CYP2C8 enzyme, exhibiting an IC50 of 4.07 μM. As a metabolite of Gemfibrozil, this compound plays a significant role in studying drug metabolism and interactions, particularly within the context of lipid metabolism and therapeutic drug monitoring. Its inhibition capacity makes it relevant for research focused on pharmacokinetics and the effects of CYP2C8 modulation on drug efficacy and safety. -
CYP2E1 Inhibitor
CYP2E1-IN-1 is a potent inhibitor of cytochrome P450 2E1 (CYP2E1) with a Kd of 7.02 μM, an IC50 of 1.64 μM, and a Ki of 0.897 μM. This compound activates the Nrf2/HO-1 signaling pathway and effectively inhibits reactive oxygen species (ROS) production, contributing to the alleviation of pancreatic injury. With significant anti-inflammatory and antioxidant properties, CYP2E1-IN-1 is suitable for research applications focused on severe acute pancreatitis and other inflammation-related diseases. -
CYP1A Inducer
β-Apo-8'-carotenal is a potent inducer of CYP1A, acting through the aryl hydrocarbon receptor (AhR) pathway. This carotenoid has demonstrated the ability to induce DNA strand breaks and lipid peroxidation in cancer cells, making it a valuable tool for research into cancer biology and metabolic disorders. Its role as a provitamin A compound further emphasizes its potential applications in studies related to cellular metabolism and disease mechanisms. -
CYP51 Inhibitor
Antifungal agent 136 is an irreversible inhibitor of fungal lanosterol 14α-demethylase (CYP51). It demonstrates potent antifungal activity against drug-resistant strains of Candida albicans and effectively downregulates IL-6 expression. This compound holds potential for research applications in the fields of fungal infection and inflammatory diseases. -
CYP2C19 Inhibitor
CYP2C19-IN-1 is a selective inhibitor of the cytochrome P450 enzyme CYP2C19, exhibiting a favorable safety profile with no hepatotoxicity or Ames test toxicity. It demonstrates potent inhibition of RNA-dependent RNA polymerase (RdRP) with a Ki value of 6.16 µM. This compound is primarily utilized in research focused on antiviral therapies against Zika virus (ZIKV). -
CYP Isozymes Inhibitor
RPR203494 is a selective inhibitor of cytochrome P450 (CYP) isozymes, with significant activity against p38 mitogen-activated protein kinase, exhibiting an IC50 of 9 nM and an EC50 of 60 nM. This compound effectively inhibits hepatic CYP enzymes, making it a valuable tool in the study of drug metabolism and pharmacokinetics. RPR203494 holds potential for research applications related to rheumatoid arthritis and other inflammatory conditions, aiding in the exploration of therapeutic strategies targeting CYP-mediated pathways. -
CYP51/PD-L1 Inhibitor
CYP51/PD-L1-IN-4 is a potent dual-target inhibitor of CYP51 and PD-L1, demonstrating IC50 values of 0.17 μM and 0.021 μM, respectively. This compound exhibits significant antifungal activity and is effective against drug-resistant fungal strains in vitro. CYP51/PD-L1-IN-4 is suitable for research applications focused on fungal infections and the interplay between fungal pathogens and immune checkpoint regulation. -
Protein kinase inhibitor
Apigenin, found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally-occurring glycosides. Apigenin acts as a monoamine transporter activator, one of the few chemicals demonstrated to possess this property. Apigenin is a ligand for central benzodiazepine receptors that competitively inhibited the binding of flunitrazepam with a Ki of 4μM, exerting anxiolytic and slight sedative effects.
- Action of clotrimazole is against the division and growing of fungi.Clotrimazole alters the permeability of the fungal cell wall and inhibits the activity of enzymes within the cell. It specifically inhibits the biosynthesis of ergosterol and other sterols required for cell membrane production.
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CYP2D6 inhibitor
Haloperidol (Haldol) is an antipsychotic and butyrophenone.
