cyp3a4

PF-4981517 (CYP3cide) is a efficient, specific and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC 50 values for CYP3A activity are 0.03 μM,17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. PF-4981517 is able to be used to distinguish the contributions of CYP3A4 versus CYP3A5 on drug Metabolism.

Verapamil hydrochloride (Verapamil HCl) is a calcium channel blocker that is a class IV anti-arrhythmia agent.

Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.

Verapamil (CP-16533-1) is a calcium channel blocker and an orally active and effective inhibitor of P-gp. Verapamil inhibits CYP3A4 and can be used in studies about the treatment of high blood pressure, heart arrhythmias, and angina research.

Tetrahydrocurcumin (HZIV 81-2), a major metabolite of curcumin, has strong antioxidant and cardioprotective properties.

Stiripentol (BCX2600) (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59 0.516 μM and IC50 of 1.58 3.29 μM, respectively.

Germacrone is extracted from Curcuma zedoaria and has anti-inflammatory, anti-androgenic and antiviral activities. It also inhibits the proliferation of glioma cells by promoting apoptosis.

TAK-715 is a p38 MAPK inhibitor for p38α.

Cletoquine is a major active metabolite of Hydroxychloroquine. Cletoquine has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune disease treatment.

1. Bergaptol (4-Hydroxybergapten) shows very good radical scavenging activity. 2. Bergaptol is a potent inhibitor of debenzylation activity of CYP3A4 enzyme.

alpha-Asarone (trans-Asarone) is a psychoactive compound with antidepressant-like activity in mice.

Rosavin (Rosavidin) has antidepressant and anxiolytic actions, helps balance all the neurotransmitters.

Chalepensin, a furanocoumarin isolated from the rutaceae plant Ruta chalepensis L., is a selective CYP2A6 inhibitor, inhibiting CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4.Chalepensin exhibits Chalepensin j has antiprotozoal activity and inhibits methicillin-resistant Staphylococcus aureus (MRSA) with MIC values in the range of 32-128 μg mL.

Norfluoxetine Hydrochloride (Norfluoxetine HCl) is an active metabolite of fluoxetine. Fluoxetine is an antidepressant drug.

CYP3A4-IN-4 (compound Δ,Λ-3) constitutes a Ru(II)-Ir(III) complex that acts as a photoactive inhibitor of the primary human drug-metabolizing enzyme CYP3A4. This complex features a [Ru(tpy)(Me2bpy)] photocaging group and exhibits an IC50 of 2.2 μM for the inhibition of microsomal CYP3A4 under irradiation conditions (λirr=530 nm, tirr=15 min). The phototherapeutic index (PI) of CYP3A4-IN-4 is 5.4.

CYP3A4-IN-1 is a potent inhibitor of cytochrome P450 3A4 (CYP3A4) (IC50: 0.085 μM).

CYP3A4-IN-3 is a specific, highly affinity cytochrome P450 3A4 (CYP3A4) (cytochrome P450 3A4 (CYP3A4)) inhibitor (IC50: 0.075 μM). CYP3A4-IN-3 is an analogue of ritonavir with a simpler structure and twice as much inhibition as ritonavir. CYP3A4-IN-3 can be used as an antiviral agent and immunosuppressant.

CYP3A4-IN-2 is a specific inhibitor of cytochrome P450 3A4 (CYP3A4) (IC50: 0.055 μM). As a ritonavir analogue with a more hydrophobic R2 side group, CYP3A4-IN-2 exhibits stronger inhibition than ritonavir and is capable of acting as an immunosuppressive and antiviral agent.

hCYP3A4-IN-1 (compound C6) is a potent, orally active inhibitor of hCYP3A4, exhibiting IC50 values of 43.93 nM in human liver microsomes (HLMs) and 153.00 nM in the CHO-3A4 stably transfected cell line. It competitively inhibits the CYP3A4-mediated hydroxylation of N-ethyl-1,8-naphthalimide (NEN) with a Ki of 30.00 nM [1].

Calf thymus DNA (DNA from calf thymus, Thymonucleic acid) is a high-quality double-stranded template DNA extracted from the bovine thymus gland, widely used in studying DNA binding anticancer agents and DNA binding agents that regulate DNA structure and function.

K777 is a potent, orally active, and irreversible inhibitor of cysteine protease, functioning as a potent CYP3A4 inhibitor (IC50 = 60 nM) and a selective CCR4 antagonist, which inhibits chemotaxis. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypanosoma cruzi, and cathepsins B and L, targeting cathepsin-mediated cell entry and exhibiting broad-spectrum antiviral activity. It inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.

RG-12525(NID 525) is an orally available, selective and competitive leukotriene D (LTD) antagonist that inhibits LTC4, LTD4 and LTE4-induced contraction of guinea pig thin-walled bands, with IC50 values of 2.6 nM, 2.5 nM, and 7 nM, respectively.RG-12525 inhibits CYP3A4, with a Ki value of 0.5 µM. RG-12525 is a novel and potent PPAR-γ agonist (IC50 value of about 60 nM) with species specificity for the study of asthma.

ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2 3 4. It is used in the research on inflammatory diseases, cancer, and AIDS.

Aβ-IN-1 is a novel, potent and orally active γ-secretase modulator (GSM). Aβ-IN-1 potently reduced Aβ42 levels with an IC 50 value of 0.091 μM in cultured cells without inhibiting CYP3A4. Aβ-IN-1 shows a sustained pharmacokinetic profile.