Antibiotics & Metabolites

GSK-1071306 is a bio-active chemical.

GSK-1268992 is a bio-active chemical.

GSK-1268997 is a bio-active chemical.

LNC-119 is an aminosteroid.

Iloperidone metabolite P95 is a metabolite of the atypical antipsychotic iloperidone . It binds to the serotonin (5-HT) receptor subtype 5-HT2A and α1-, α2B-, and α2C-adrenergic receptors with mean Ki values of 7.08, 21.38, 83.18, and 47.86 nM, respectively, but does not cross the blood-brain barrier.

Imidafenacin metabolite M4 is a metabolite of the muscarinic acetylcholine receptor antagonist imidafenacin.1It is formed from imidafenacin by the cytochrome P450 (CYP) isoform CYP3A4.

Avanafil metabolite M4 is a major active metabolite of the phosphodiesterase 5 (PDE5) inhibitor avanafil . Avanafil is metabolized by the cytochrome P450 (CYP450) isoforms CYP3A4 and CYP2C to the major metabolites avanafil metabolite M4 and avanafil metabolite M16 , as well as minor metabolites. Avanafil metabolite M4 inhibits PDE5 with 18% of the potency of avanafil.

Antibiotic PF 1052 is a fungal metabolite originally isolated from Phoma.1,2 It is active against S. aureus, S. parvulus, and C. perfringens (MICs = 3.13, 0.78, and 0.39 μg/ml, respectively), among others.1 It inhibits neutrophil migration in a wound assay using zebrafish larvae expressing GFP-labeled neutrophils, reducing pseudopodia formation and inducing rounding of neutrophils.2 Antibiotic PF 1052 is selective for neutrophil migration over macrophage migration in zebrafish larvae. It also inhibits the migration of murine neutrophils when used at concentrations of 10 and 20 μM.

Norimatinib mesylate, also known as N-Desmethyl imatinib mesylate, is a metabolite derived from Imatinib, which acts as a potent multi-target inhibitor of v-Abl, c-Kit, and PDGFR.