hydroxylation

Liarozole (R75251 dihydrochloride) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.

Worenine (Worenin) is used in the a flurophore switched probe which aids in correction of an abasic site (AP site) caused by the removal of a damaged base in DNA.

2,4-DPD is competitive inhibitor of the oxygen-sensing enzyme HIF-α prolyl hydroxylase (HIF-PH)

1,4-DPCA is an inhibitor of prolyl-hydroxylase with an IC50 of 2.4 µM for collagen hydroxylation in human foreskin fibroblasts and 60 μM for factor inhibiting HIF (FIH).

Ifosfamide (NSC-109724) alkylates and forms DNA crosslinks, thereby preventing DNA strand separation and DNA replication. Ifosfamide is a synthetic analog of the nitrogen mustard cyclophosphamide with antineoplastic activity. This agent is a prodrug that must be activated through hydroxylation by hepatic microsomal enzymes.

iron chloride hexahydrate promoted selective hydroxylation and chlorination of benzyl ketone derivatives for the construction of hetero-quaternary scaffolds.

VH-298 is a potent inhibitor of VHL that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, that is the blockade of the VHL:HIF-α protein-protein interaction downstream of HIF-α hydroxylation by PHD enzymes.

Calcifediol-D6 is the deuterated form of Calcifediol (TMSM-3156), which is a prehormone that is produced in the liver by hydroxylation of vitamin D3 by the enzyme cholecalciferol 25-hydroxylase.

FG 7142 (LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex. FG 7142 , a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM).

L-hydroxylysine dihydrochloride , is formed by posttranslational hydroxylation of some lysine residues. It is an amino acid, is exclusive to collagen protein.

(24S)-24,25-Dihydroxyvitamin D3 undergoes multiple hydroxylation processes to form active vitamin D3 analogs.

Diethyl bipy55'DC inhibits CP4H activity in cultured cells. The stability of collagen relies on post-translational modifications, the most prevalent being the hydroxylation of collagen strands by collagen prolyl 4-hydroxylases.

YZN62564, also known as meso-Tetra(2,6-dimethoxyphenyl) porphine, is a synthetic porphyrin compound with supramolecular characteristics. With Fe and Mn as central atoms, YZN62564 serves as a catalyst for various epoxidation and hydroxylation reactions.

Docarpamine is an orally active dopamine prodrug that is converted into active dopamine in the small intestine and liver through hydroxylation. In situations of spontaneous hypertension, it primarily activates peripheral D1-like receptors (D1-like receptor) to lower blood pressure and heart rate. Under normal blood pressure conditions, Docarpamine exhibits pressor effects and tachycardia by activating D1-like receptors, vasopressin V1 receptors (vasopressin V1 receptor), and α-adrenergic receptors (α-adrenergic receptor). Docarpamine is useful for studying renal vasodilation and diuresis.

Tenuifoliside C, isolated from Polygala tenuifolia Willd, is a targeted lactate dehydrogenase inhibitor that significantly inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1[1].

Licodione is a Cytochrome P450 Monooxygenase Catalyzing 2-Hydroxylation of 5-Deoxyflavanone.

Metyrapol is a competitive inhibitor of 11-deoxycorticosterone hydroxylation by 11β-hydroxylase.

Epmedin C (Baohuoside-VI) was metabolized via desugarization, dehydrogenation, hydrogenation, dehydroxylation, hydroxylation, demethylation and glucuronidation pathways in vivo. It has potential activity against osteoporosis by stimulating osteoblasts.

MeIQx (MeIQx) is a food-derived carcinogen that has been found in high temperature-cooked fish and meats.1It is activated by hydroxylation and subsequent O-acetylationviathe cytochrome P450 (CYP) isoform CYP1A2 and N-acetyltransferase 2, respectively, in UV5 cells expressing the human enzymes to a metabolite that reacts with DNA to form adducts.2MeIQx (200 and 400 ppm in the diet) induces tumor formation in rats.3

5-hydroxy Propranolol is a metabolite of propranolol , a β-adrenergic receptor antagonist. Propranolol is primarily metabolized in the liver, with cytochrome P450 isoform 2D6 directing ring hydroxylation and the generation of 5-hydroxy propranolol and related metabolites.

L-Tyrosine-13C9,15N is intended for use as an internal standard for the quantification of L-tyrosine by GC- or LC-MS. L-Tyrosine (T0493) is a non-essential amino acid.1It is produced by hydroxylation of phenylalanine by phenylalanine hydroxylase but can also be obtained from dietary sources or degradation of endogenous proteins, resulting in L-tyrosine release.1,2L-Tyrosine is a precursor in the biosynthesis of catecholamine neurotransmitters, melanins, and thyroid hormones.3Plasma, skeletal muscle, and erythrocyte levels of L-tyrosine are decreased in patients with chronic kidney disease.1

(R)-Omeprazole is the inactive isomer of omeprazole , a gastric proton-pump inhibitor. A stereoselective hydroxylation of (R)-omeprazole is mediated primarily by cytochrome P450 (CYP) 2C19, whereas CYP3A4 favors sulfoxidation of the active (S)-enantiomer . (R)-Omeprazole has been shown to act as a reversible direct-acting and metabolism-dependent inhibitor of CYP2C19 in pooled human liver microsomes (IC50 = 8.1 μM).

21-Deoxycortisol is a corticosteroid metabolite of 17-hydroxyprogesterone produced in the adrenal glandvia11-hydroxylation by 11β-hydroxylase.1,2Serum levels of 21-deoxycortisol are elevated in patients with congenital adrenal hyperplasia that are heterozygous for mutations inCYP2A21, the gene encoding steroid 21-hydroxylase, and have been used as a biomarker for the detection of 21-hydroxylase deficiencies. 1.Fiet, J., Villette, J.-M., Galons, H., et al.The application of a new highly-sensitive radioimmunoassay for plasma 21-deoxycortisol to the detection of steroid-21-hydroxylase deficiencyAnn. Clin. Biochem.31(Pt. 1)56-64(1994) 2.Cristoni, S., Cuccato, D., Sciannamblo, M., et al.Analysis of 21-deoxycortisol, a marker of congenital adrenal hyperplasia, in blood by atmospheric pressure chemical ionization and electrospray ionization using multiple reaction monitoringRapid Commun. Mass Spectrom.18(1)77-82(2004)

Polygalaxanthone III can significantly inhibit chlorzoxazone 6-hydroxylation catalyzed by CYP2E1.