Cytochrome P450 Inhibitor

Paramethasone Acetate (Standard) is the analytical standard of Paramethasone Acetate (HY-107939). This product is intended for research and analytical applications. Paramethasone Acetate is an orally active long-acting glucocorticoid. Paramethasone Acetate directly inhibits testicular aromatase, thereby reducing the synthesis of estradiol. Paramethasone Acetate suppresses the basal and midcycle luteinizing hormone surges in female animals and blocks estrogen synthesis. Paramethasone Acetate also decreases circulating levels of dihydrotestosterone, androstenedione and estradiol in male animals. Paramethasone Acetate inhibits cartilage degeneration and alleviates joint pathological damage in osteoarthritis models. Paramethasone Acetate can be used in research related to osteoarthritis and endocrinology.

LP8 is a Pyridinyl-type CYP51 inhibitor and can be used for study of chagas disease and American trypanosomiasis.

(Rac)-Ketoconazole ((Rac)-R 41400) is an antifungal imidazole compound with oral activity. (Rac)-Ketoconazole interferes with ergosterol synthesis by inhibiting cytochrome P450-dependent 14α-sterol demethylase (CYP51), a key enzyme on the fungal cell membrane, leading to membrane dysfunction and ultimately inhibition of fungal growth and reproduction. (Rac)-Ketoconazole is indicated for studies of fungal infections.

2-Pentylbenzimidazole (Compound 10f), benzimidazole derivative, is an aminopyrine N-demethylase inhibitor with a pIC₅₀ of 4.3. 2-Pentylbenzimidazole can be used for the researches of cancer and metabolic disease.

Aspergillusidone F is a Depsidone and antibacterial agent. Aspergillusidone F can be isolated from a marine fungus Aspergillus unguis. Aspergillusidone F potently inhibits Aromatase with an IC₅₀ of 0.5 μM. Aspergillusidone F exhibits antibacterial activity against Pseudomonas aeruginosa and Methicillin (HY-121544)-resistant Staphylococcus aureus. Aspergillusidone F exhibits potent larvicidal activity against Artemia salina larvae, with an LC₅₀ value of 12.8 μM. Aspergillusidone F exhibits anticancer activity against intrahepatic cholangiocarcinoma, non-small cell lung cancer, and acute lymphoblastic leukemia.

Methoxsalen (Standard) is the analytical standard of Methoxsalen. This product is intended for research and analytical applications. Methoxsalen (8-Methoxypsoralen) is a furanocoumarin compound used in psoralen, used in studies of psoriasis, eczema, vitiligo and some sun-exposed cutaneous lymphomas, and is a P450 inhibitor.

SMA-245 is an inhibitor of Filovirus glycoproteins, acting on Ebola virus (EBOV) and Marburg virus (MARV). SMA-245 blocks the endosomal membrane fusion step of filoviruses by binding to the EBOV GP1/GP2 fusion loop. SMA-245 inhibits MARV viral entry. SMA-245 can be used in research related to filovirus infections.

E-2101 is a novel antispastic agent. E-2101 is a competitive CYP2C19 and CYP2D6 inhibitor with K_i values of 15 and 48 μM, respectively. E-2101 is metabolized by Cytochromes P450 to form monohydroxylated (M1 and M2), dihydroxylated (M3), and N-dealkylated metabolites (M4). E-2101 can be used in the research of skeletal muscle spasm.

LY113174 is an orally active aromatase inhibitor (IC₅₀ = 24 nM). LY113174 blocks testosterone induced increase in uterine weight in rat, and inhibits ovarian estrogen biosynthesis.

Gemfibrozil-d6-1 (CI-719-d6-1) is the deuterium labeled Gemfibrozil (HY-B0258). Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with K_i values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.

Polygalaxanthone III (Standard) is the analytical standard of Polygalaxanthone III (HY-N1407). This product is intended for research and analytical applications. Polygalaxanthone III is a representative xanthone component of Polygala tenuifolia. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1, with an IC₅₀ of 50.56 μM. Polygalaxanthone III repairs skin damage induced by M. furfur via activating STAT3 phosphorylation and exerts anti-inflammatory effects. Polygalaxanthone III can be used for research on M. furfur-related skin damage.

Nefazodone (Standard) is the analytical standard of Nefazodone. This product is intended for research and analytical applications. Nefazodone is an orally active phenylpiperazine antidepressant. Nefazodone can potently and selectively block postsynaptic 5-HT2A receptors, and moderately inhibit 5-HT and noradrenaline reuptake. Nefazodone can also relieve the adverse effects of stress on the the immune system of mice. Nefazodone has a high affinity for CYP3A4 isoenzyme, which indicates that it has certain risk of agent-agent interaction.

SDZ-285604 (VNF) is a T. cruzi CYP51 inhibitor and can be used for study of Trypanosoma cruzi infection.

CYP51-IN-25 is a orally active broad spectrum antifungal agent with the MIC₈₀ of 0.00625-0.05 μg/mL. is a CYP51-IN-25 is a deuterated compound with antibiotic properties. CYP51-IN-25 can inhibit the fungal CYP51 enzyme, block ergosterol synthesis, and disrupt cell membrane integrity. CYP51-IN-25 can be used for research on fungal infections.

Arasertaconazole is a potent 14α-lanosterol demethylase inhibitor. Arasertaconazole has antifungal and antibacterial activity.

SR-2555 (NSC 314055) is a CYP2D6 inhibitor with an IC₅₀ of 1017 μM against human CYP2D6. SR-2555 inhibits the AMMC demethylase activity of recombinant CYP2D6; differentially enhances the sensitivity of hypoxic cells to the lethal effect of γ-rays; and exhibits cytotoxicity against hypoxic cells. SR-2555 can be used in cancer-related research.

TUPS can inhibit the gene expression of epoxide hydrolase (sEH) and cytochrome P450 (CYP). TUPS can be used in cardiovascular disease-related research.

Gentiopicroside (Standard) is the analytical standard of Gentiopicroside. This product is intended for research and analytical applications. Gentiopicroside, a naturally occurring iridoid glycoside, inhibits P450 activity, with an IC50 and a Ki of 61 μM and 22.8 μM for CYP2A6; Gentiopicroside has anti-inflammatoryand antioxidative effects.

CYP3A4-IN-4 (compound Δ,Λ-3), a Ru(II) Ir(III) Conjugate, is a photoactive inhibitor of the major human drug metabolizing enzyme CYP3A4. CYP3A4-IN-4 containing the [Ru(tpy)(Me2bpy)] photocaging group showed an IC₅₀ of 2.2 μM for inhibition of microsomal CYP3A4 under light conditions (λirr=530 nm, tirr=15 min).

Clomethiazole (Standard) is the analytical standard of Clomethiazole. This product is intended for research and analytical applications. Chlormethiazole is an potent and orally active GABAA agonist. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus.