cytochromes

1-Ethynylpyrene is an aryl acetylenic inhibitor of CYTP450 1A1 (IC50 = 0.18 μM), 1A2 (IC50 = 0.32 μM), and 2B1 (IC50 = 0.04 μM).

Tauroursodeoxycholate (UR 906), also known as ursodoxicoltaurine, is a highly hydrophilic tertiary bile acid that is produced in humans at a low concentration. Tauroursodeoxycholate is the more hydrophilic form of ursodeoxycholic acid, which is the more abundant naturally produced bile acid in humans.Tauroursodeoxycholate is being investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.

ACP-5862 is a major active and pyrrolidine ring-opened metabolite of Acalabrutinib (IC50: 5.0 nM for BTK). Acalabrutinib is an irreversible and highly selective BTK inhibitor (IC50: 3 nM; EC50: 8 nM).

Androsta-1,4,6-triene-3,17-dione is a lipophilic and specific aromatase inhibitor (Ki: 0.18 μM) that inhibits estrogen biosynthesis, exhibits antifertility effects, and induces impairment of spatial memory.

Antihistamine-1 is an H1-antihistamine (Ki: 6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel (IC50s: 5.4 and 0.8 μM).

CYP11B2-IN-1 is an effective and selective inhibitor of CYP11B2 with IC50s of 2.3 nM and 142 nM for CYP11B2 and CYP11B1.

CYP17-IN-1 is an effective oral inhibitor of CYP17 that can inhibit CYP17 in rats and humans with IC50 of 15.8 and 20.1 nM.

PC945 (Opelconazole) is a potent broad-spectrum antifungal compound with inhibitory effect on fumonisinol 14α-demethylase (CYP51A/CYP51B), which can be used in the study of fungal infections of the lungs.

Seviteronel R enantiomer (VT-464 R enantiomer) is a Seviteronel isomer produced during the manufacturing process.

Seviteronel (VT-464) is a novel CYP17 cleavage enzyme inhibitor and androgen receptor antagonist used in breast and prostate cancer research.

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.

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.

Phortress (NSC-710305) is a potent AhR ligand with strong binding affinity, which subsequently triggers the transcription of CYP1A1 and induces antitumor activity.

Azalanstat (RS 21607) is an orally available selective mammalian lanosterol 14-alpha-demethylase inhibitor with hypocholesterolemic activity that inhibits cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes, and hamster livers through inhibition of the cytochrome P450 enzyme, lanosterol 14 alpha demethylase.

Vorozole (R83842) is an orally active, potent, and selective nonsteroidal aromatase inhibitor.Vorozole exhibits antitumor activity in vivo and may be used in the study of breast cancer.

(-)-Vorozole is an orally active non-steroidal aromatase inhibitor with potency and selectivity. (-)-Vorozole has demonstrated antitumor activity in in vivo experiments. (-)-Vorozole is used in the study of breast cancer.

Finrozole (MPV 2213ad) is a novel selective aromatase inhibitor that is partially reversible for breast development.

Inz-1 is an effective and fungal-selective inhibitor of mitochondrial cytochrome bc1 with IC50s of 8.092 and 45.320 μM for yeast and human. Inz-1 reverses Fluconazole or other triazole antifungals' resistance in the pathogenic fungus Candida albicans.

EN3356 is an orally available and selective inhibitor of steroidal 17-alpha-hydroxylase/C17,20 cleavage enzyme (CYP17A1 or CYP17), a non-steroidal cleavage enzyme-selective compound with potential anti-androgenic and anti-tumor activity.

MS-PPOH is a potent and selective inhibitor of cytochrome P450 (CYP) epoxygenase, specifically inhibiting CYP2C8 and CYP2C9 with IC50 values of 15 and 11 µM, respectively.

CYP1B1-IN-1 is a selective and highly potent cytochrome P450 1B1 (CYP1B1) inhibitor with potential anticancer and antitumor activity for breast cancer research.

Cholesterol 24-hydroxylase-IN-1 is an orally active, selective, and potent inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1) that crosses the blood-brain barrier.Cholesterol 24-hydroxylase-IN-1 may be useful in the study of epilepsy-like neurological disorders. Cholesterol 24-hydroxylase-IN-1 is used to study epilepsy-like neurological diseases.

Endoxifen hydrochloride, a principal active metabolite of Tamoxifen (TAM), exhibits heightened affinity and specificity towards the estrogen receptor and possesses aromatase inhibitory capability. It holds promise for breast cancer research.