Cytochrome P450 Inhibitor

Buthiobate (S-1358) is a fungicide. Buthiobate is a cytochrome P-450 inhibitor with an IC₅₀ of 0.4 μM. Buthiobate binds to the heme iron of cytochrome P-450 (low-spin state) via its pyridine group, thereby blocking the initial hydroxylation of the 14α-methyl group. Buthiobate is used in research on powdery mildew in agricultural and horticultural crops.

Liarozole (dihydrochloride) (Standard) is the analytical standard of Liarozole (dihydrochloride). This product is intended for research and analytical applications. Liarozole (R75251) dihydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole dihydrochloride inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of RA (IC50=7 μM), resulting in increased tissue levels of RA. Liarozole dihydrochloride shows antitumoral properties.

Abiraterone acetate-d₃ (CB7630-d₃) is deuterium labeled Abiraterone acetate. Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598).

Dronedarone (Standard) is the analytical standard of Dronedarone. This product is intended for research and analytical applications. Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4.

Fluxapyroxad (Standard) is the analytical standard of Fluxapyroxad. This product is intended for research and analytical applications. Fluxapyroxad is a synthetic broad-spectrum fungicide for the control of fungal diseases. It works by inhibiting succinate dehydrogenase in complex II of the mitochondrial respiratory chain, resulting in inhibition of spore germination, germ tubes and mycelia growth within the fungus target species.

Exemestane-d₄ (FCE 24304-d₄) is deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC₅₀s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research.

GNF7686 is a cytochrome b inhibitor. GNF7686 exhibits inhibitory activity against complex III in the extracts of L. donovani and T. cruzi.

4-Methoxywarfarin (compound 15) is a racemic inhibitor of cytochrome P450 2C9 (CYP2C9). 4-Methoxywarfarin inhibits CYP2C9-catalyzed S-warfarin 7-hydroxylation with a K_i of 11 μM. 4-Methoxywarfarin is applicable to studies related to CYP2C9 inhibition, warfarin metabolism, and the structure-activity relationship of CYP2C9 inhibitors.

Fomepizole (Standard) is the analytical standard of Fomepizole. This product is intended for research and analytical applications. Fomepizole (4-Methylpyrazole) is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning.

Cobicistat (Standard) is the analytical standard of Cobicistat. This product is intended for research and analytical applications. Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) enzymes with IC₅₀s of 30-285 nM. Cobicistat is a pharmacokinetic enhancer which increases the overall absorption of several HIV medications.

ACP-5862-d₄ is deuterium labeled ACP-5862. ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC₅₀ of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC₅₀ of 3 nM and EC₅₀ of 8 nM.

Exemestane-d₃ is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC₅₀s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research.

2-(Isopentylamino)naphthalene-1,4-dione (compound 3d), a Vitamin K (HY-B2172) analogue, shows protection in Pentylenetetrazole (PTZ)-induced seizure model. 2-(Isopentylamino)naphthalene-1,4-dione significantly increases ATP levels in zebrafish as well as HT-22 cells. 2-(Isopentylamino)naphthalene-1,4-dione shows excellent permeability into the brain.

CD-6 is a flavonoid CYP2A6 inhibitor (IC₅₀: 1.566 μM). CYP2A6 inhibits the metabolism of nicotine to cotinine, resulting in an increase in the amount of nicotine available in the blood, leading to increased smoking behavior. CD-6 mediates CYP2A6 inhibition and can be used in research on smoking cessation or smoking-related diseases.

Oteseconazole (Standard) is the analytical standard of Oteseconazole. This product is intended for research and analytical applications. Oteseconazole (VT-1161) is a potent and orally active anti-fungal agent. Oteseconazole potently binds to and inhibits Candida albicans cytochrome P45051 (CYP51) activity (K_d ≤39 nM), shows no obvious effect on human CYP51. Oteseconazole also can be used for the research of dermatophytes.

Antifungal agent 137 (Compound 4S) is an antifungal agent. Antifungal agent 137 inhibits Phomopsis sp. (PS), with an EC₅₀ of 0.15 μg/mL. Antifungal agent 137 inhibits lanosterol 14α-demethylase (CYP51), with an IC₅₀ of 5.00 μg/mL. Antifungal agent 137 disrupts the morphology of PS mycelia, impairs cell membrane integrity, and induces an increase in intracellular ROS levels, triggering oxidative stress. Antifungal agent 137 can be used for the study of fungal infection.

Topiroxostat (Standard) is the analytical standard of Topiroxostat. This product is intended for research and analytical applications. Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC₅₀ value of 5.3 nM and a K_i value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment.

Atazanavir (Standard) is the analytical standard of Atazanavir. This product is intended for research and analytical applications. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.

Dronedarone-d₆ (SR 33589-d₆) is deuterium labeled Dronedarone. Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4.

Simmitecan is a potent topoisomerase I (TOP1) inhibitor, which is a 9-substituted lipophilic camptothecin (Camptothecin (HY-16560)) derivative. Simmitecan blocks DNA replication and transcription, thereby inducing tumor cell apoptosis by inhibiting the activity of TOP1. Simmitecan can be used in the research of cancers such as liver cancer.