Cytochrome P450 Substrate

HN0037 is a selective, orally active Helicase-primase inhibitor. HN0037 is mainly metabolized by CYP3A4. HN0037 inhibits HSV replication by targeting the viral helicase-primase complex, which consists of three proteins encoded by UL5 (helicase), UL52 (primase), and UL8 (scaffold protein that promotes primer synthesis).

20-Hydroxyvitamin D3 (20(OH)D3), a product of vitamin D3 hydroxylation, is a noncalcemic immunomodulator. 20-Hydroxyvitamin D3 binds to vitamin D receptor (VDR), activates VDR and aryl hydrocarbon receptor (AhR) signaling, stimulates CYP24A1 expression, and drives VDR nuclear translocation. 20-Hydroxyvitamin D3 inhibits NF-κB activity via IκBα upregulation. 20-Hydroxyvitamin D3 acts as a substrate for CYP27B1 and rat CYP24A1, undergoing hydroxylation to form dihydroxy-derivatives. 20-Hydroxyvitamin D3 inhibits cell proliferation, colony formation, migration, and tumor growth, and induces cell differentiation in cancer cells. 20-Hydroxyvitamin D3 can be used for the research of inflammatory and autoimmune diseases, melanoma, breast carcinomas, and hepatocarcinoma.

(±)5(6)-EET Ethanolamide is a metabolite of Anandamide (HY-10863) generated via oxidation by cytochrome P450 enzymes. (±)5(6)-EET Ethanolamide is also a selective cannabinoid receptor 2 (CB2) agonist. (±)5(6)-EET Ethanolamide has K_i values of 11.4 μM and 8.9 nM for human CB1 and CB2, respectively . (±)5(6)-EET Ethanolamide can be used in research on immunomodulation and neuroinflammation.

CP-506 (compound 26) is an anticancer compound and a substrate for nitroreductase and CYP oxidoreductases. CP-506 has anticancer activity.

G256 is a cytochrome P450 substrate with antiarrhythmic properties. In recombinant monooxygenase systems, G256 undergoes N-hydroxylation of the terminal aminoguanidine nitrogen, as well as ring hydroxylation catalyzed by cytochrome P4502C3. G256 generates N-hydroxyaminoguanidine metabolites via N-hydroxylation in liver microsomal fractions. G256 produces phenol metabolites through ring hydroxylation in both liver microsomal fractions and recombinant cytochrome P450 systems. G256 can be used for research on arrhythmias.

Anticancer agent 318 (Compound 8 (6)) is a selective anticancer agent. Anticancer agent 318 can be metabolized by CYP1A1, CYP1A2 and CYP1B1. After bioactivation, Anticancer agent 318 exerts antiproliferative activity in breast cancer cells expressing CYP1. Anticancer agent 318 can be used in the research of breast cancer.

2-Hydroxymelatonin is a major hydroxylated metabolite of Melatonin (HY-B0075). It is enzymatically produced in plants by melatonin 2-hydroxylase (M2H/AsMT), while in animals, it is generated in trace amounts via CYP450 or spontaneous oxidation. 2-Hydroxymelatonin acts as a respiratory burst oxidase homolog (RBOH)-dependent ROS burst inducer, thereby regulating stress tolerance, seed germination and growth in plants. In animal cells, 2-Hydroxymelatonin synergizes with BMP-4 to promote osteogenesis, and exerts pro-apoptotic and anti-metastatic activities against colorectal cancer cells. 2-Hydroxymelatonin can be used in studies related to plant premature senescence, osteoporosis and colorectal cancer.

3-N-Nitroso-N-methylaminopyridine is a non-carcinogenic, non-mutagenic arylalkyl nitrosamine isomer that serves as a substrate for enzymatic metabolic processes. 3-N-Nitroso-N-methylaminopyridine undergoes enzymatic denitrosation, enzymatic N-oxide formation, and limited oxidative demethylation to produce trace amounts of 3-hydroxypyridine. 3-N-Nitroso-N-methylaminopyridine directly induces gene mutations in E. coli, but its mutagenic potential is eliminated by the rodent liver S-100 fraction. 3-N-Nitroso-N-methylaminopyridine shows no carcinogenicity in rats and no mutagenicity in the Ames test. 3-NMPY can be used in studies related to the metabolism and carcinogenic mechanisms of nitrosamine compounds in vitro and in vivo.

Desethylamiodarone (N-Desethylamiodarone; LB 33020) is the major active metabolite of Amiodarone (HY-14187) generated via CYP3A4 metabolism. Desethylamiodarone downregulates p‑Akt, p‑Bad and Bcl‑2, upregulates Bax, promotes mitochondrial release of cytochrome c, activates caspase‑3 and cleaves PARP‑1, thereby inducing cell cycle arrest and apoptosis. Desethylamiodarone can be used in cervical cancer-related research.

BI-11634 is an orally active factor Xa inhibitor and a CYP3A4 substrate. The apparent K_m values for BI-11634 metabolism are 23 μM in human liver microsomes (HLMs) and 7.6 μM with recombinant CYP3A4. BI-11634 can be used for thromboembolic disease and CYP3A4-mediated drug metabolism research.

Mono(2-ethyl-5-oxohexyl) phthalate-d₄ (MEOHP-d₄; 5-oxo-MEHP-d₄) is the deuterated-labeled Mono(2-ethyl-5-oxohexyl) phthalate (HY-133676). Mono (2-ethyl-5-oxohexyl) phthalate (MEOHP; 5-oxo-MEHP) is a secondary metabolite produced by cytochrome P450 enzyme-mediated oxidation of di(2-ethylhexyl) phthalate. Exposure levels of Mono (2-ethyl-5-oxohexyl) phthalate are associated with late-onset hypogonadism. Mono (2-ethyl-5-oxohexyl) phthalate can be used for research on mechanisms related to male reproductive endocrine disorders.

Tolterodine (tartrate) (Standard) is the analytical standard of Tolterodine tartrate. This product is intended for research and analytical applications. Tolterodine ((R)-(+)-Tolterodine) is a mAChR inhibitor and substrate for cytochrome P450 enzymes. Tolterodine competitively binds acetylcholine, reduces sympathetic excitation, and inhibits involuntary bladder muscle contraction. Tolterodine restores the Nrf2/NF-κB signaling pathway, mediates protection against inflammatory response and ferroptosis. Tolterodine ameliorates LPS (HY-D1056)-induced reactive oxygen species production and lipid oxidation. Tolterodine can be used for the research of urinary tract infections and overactive bladder.

Veratrole-d₆ is the deuterium labeled Veratrole. Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii.

11-Ketoprogesterone (11KP4) is the substrate for CYP17A1 and 11β-HSD2 that could be metabolized to 21-deoxycortisone (21dE) and 21-deoxycortisol (21dF) with glucocorticoid activity.

Desethylamiodarone-d₄ hydrochloride (N-Desethylamiodarone-d₄ hydrochloride; LB 33020-d₄ hydrochloride) is the deuterated-labeled Desethylamiodarone hydrochloride (HY-130353). Desethylamiodarone hydrochloride (N-Desethylamiodarone hydrochloride; LB 33020 hydrochloride) is the major active metabolite of Amiodarone (HY-14187) generated via CYP3A4 metabolism. Desethylamiodarone hydrochloride downregulates p‑Akt, p‑Bad and Bcl‑2, upregulates Bax, promotes mitochondrial release of cytochrome c, activates caspase‑3 and cleaves PARP‑1, thereby inducing cell cycle arrest and apoptosis. Desethylamiodarone hydrochloride can be used in cervical cancer-related research.

Desoximetasone-d₃ is the deuterium labeled Desoximetasone (HY-17570). Desoximetasone is a corticosteroid and a substrate of cytochrome P450 3A4. Desoximetasone has anti-inflammatory, anti-allergic, and immunosuppressive effects. Desoximetasone can be used in the research of various skin diseases, such as skin allergies, atopic dermatitis, and psoriasis.

Prothipendyl is a tricyclic azaphenothiazine neuroleptic agent. Prothipendyl is a substrate of the CYP isozymes CYP1A2, CYP2D6, CYP2C19 and CYP3A4. Prothipendyl has sedating and psychomotorically damping effects. Prothipendyl can be used for psychomotoric agitation, sleep disorder and anxiety research .

Desoximetasone (Standard) is the analytical standard of Desoximetasone (HY-17570). This product is intended for research and analytical applications. Desoximetasone is a corticosteroid and a substrate of cytochrome P450 3A4. Desoximetasone has anti-inflammatory, anti-allergic, and immunosuppressive effects. Desoximetasone can be used in the research of various skin diseases, such as skin allergies, atopic dermatitis, and psoriasis.

Veratrole (Standard) is the analytical standard of Veratrole. This product is intended for research and analytical applications. Veratrole (1,2-Dimethoxybenzene) is a key compound that widely exists in plants and attracts pollinators. The release of Veratrole has a circadian rhythm and plays an important role in plant reproduction, species differentiation, and interactions with pollinators. In addition, Veratrole can be demethylated by cytochrome P-450 in Streptomyces setonii.

Echihumiline is an alkaloid targeting hepatic cytochrome P450 enzymes (CYP450). Echihumiline induces DNA cross-linking and oxidative stress in hepatocytes, leading to liver necrosis and fibrosis. Echihumiline is promising for research of liver diseases.