Antibiotics & Metabolites

PSI-6206 13CD3 is the deuterium labeled PSI-6206. PSI-6206 is a potent and selective HCV NS5B polymerase inhibitor.

Ketopioglitazone is an active metabolite of pioglitazone.

Ticagrelor metabolite M5 (T437700) is a metabolite of Ticagrelor, the first reversible oral antagonist of P2Y12 receptor. Compared to Clopidogrel, Ticagrelor has faster and more consistent inhibition on ADP-receptors. Ticagrelor is used in the treatment of acute coronary syndromes (ACS).

Axitinib sulfoxide is a major metabolite of Axitinib, which is a VEGFR tyrosine kinase inhibitor and may be useful in cancer therapy.

Omeprazole sulfide (Ufiprazole), a metabolite of Omeprazole, functions as a proton pump inhibitor.

Activity: Antibiotic . Function/Pharmacology: Mupirocin is a topical antibiotic/antibacterial.1 It inhibits isoleucyl-tRNA synthase. High level mupirocin resistance was found in 8.2% of Staphylococcus aureus and 15.6% of coagulase-negative staphylococci with high level resistance being more common in methicillin-sensitive S. aureus in comparison with methicillin-resistant S. aureus.2

Activity: Endogenous cholesterol metabolite . Function/Pharmacology: 24(S)-Hydroxycholesterol is an important cholesterol metabolite (cholesterol 24-hydroxylase) found in the brain.1 It is an endogenous agonist of the nuclear receptor LXR.2 It has been shown to induce cell death in neuroblastoma cells3, possibly via a necroptosis pathway4. 24(S)-Hydroxycholesterol has also been found to be a high affinity ligand for RORα and RORγ (Ki = 25 nM).5 24(S)-Hydroxycholesterol levels are elevated in the cerebral spinal fluids of patients with neurogenerative diseases suggesting possible clinical applications.6,7 It was also able to reduce Aβ production and increase ER-resident immature amyloid precursor protein (APP) levels in human neuroblastoma SH-Sy5Y cells and CHO cells via inhibition of intracellular amyloid precursor protein trafficking.7

Activity: Antibiotic and FOXM1 inhibitor . Function/Pharmacology: Novel cyclopeptide antibiotic. Blocks bacterial protein synthesis by inhibition of mRNA-tRNA translocation by GTPase elongation factor G (EF-G), EF-TU(GTP)-catalyzed aa-tRNA delivery as well as the activity of initiation factor-1 (IF-2)1-2. Displays antitumor activity. Induces apoptosis and cell cycle arrest in various tumor cells via downregulation of FOXM1 expression3. Chemical Name: Fermentation product from Streptomyces azureus

Activity: Macrolide antibiotic; Cytochrome P450 inhibitor . Function/Pharmacology: Macrolide antibiotic. Inhibits cytochrome P450 (IC50 = 0-5 µM), thus blocking CYP450-dependent drug oxidation.