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.

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

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

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.

TAK-715 is a p38 MAPK inhibitor for p38α.

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

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

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

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

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

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-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.

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.

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.

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.

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.

Laromustine (VNP40101M) is a sulfonyl hydrolytic alkylating prodrug used in cancer therapy with significant anticancer activity. Inhibiting thioredoxin reductase can be used to study acute myeloid leukemia.

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.

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.

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.

Cepharanthine (NSC-623442) is a natural alkaloid that inhibits TNF-α-mediated NFκB stimulation, plasma membrane lipid peroxidation, and platelet aggregation, as well as cytokine production. Cepharanthine exhibits anti-inflammatory, antioxidant, and antitumor activities.

Cedrol is a cedrane sesquiterpenoid and a tertiary alcohol,Cedrol inhibits the cytochrome P450 (CYP) isoforms CYP2B6 and CYP3A4 (Kis = 0.9 and 3.4 μM, respectively)