| Hazard Information | Back Directory | [Description]
BAY-069 is a BCAT1/2 Inhibitor and Chemical Probe. BAY-069 displays high cellular activity and very good selectivity. BAY-069 displays high cellular activity. Its overall in vivo pharmacokinetic profile and its selectivity in various in vitro panels suggest that BAY-069 is suitable for in vivo experiments. Note: BAY-069 is the more active atropisomer with M-helical with IC50 of 31 nM (BCAT1), while the other atropisomer has only micromolar activity. BAY-771 is the negative control for BAY-609. | [Uses]
BAY-069 is a potent branched-chain amino acid transaminases 1 (BCAT1) and BCAT2 inhibitor with IC50 values of 31 nM and 153 nM, respectively. BAY-069 also can be used as a chemical probe. BAY-069 can be used tor research anticancer[1]. | [in vivo]
BAY-069 exhibits high metabolic stability after incubation with human liver microsomes (CLblood = 0.11 L/h/kg) and moderate metabolic stability after incubation with rat hepatocytes (CLblood = 1.8 L/h/kg); shows high permeability through Caco-2 cell monolayers with no hint of efflux[1].
BAY-069 (0.3 mg/kg for i.v.; 0.6 mg/kg for p.o.; single dosage) exhibits a favorable pharmacokinetic profile after i.v. dosing with low blood clearance (CLblood), moderate volume of distribution at steady state (Vss), and intermediate terminal half-life (t1/2). | Animal Model: | Male Wistar rats[1] | | Dosage: | 0.3 mg/kg for i.v.; 0.6 mg/kg for p.o. | | Administration: | i.v. or p.o.; single dosage | | Result: | Pharmacokinetic Parameters of BAY-069 in male Wistar rats[1].
| CLblood (L/h/kg) | Vss (L/kg) | t1/2 (h), i.v. | AUCnorm (kg·h/L), i.v. | AUCnorm (kg·h/L), p.o. | F (%), p.o. | | 0.64 | 0.25 | 1.6 | 2.9 | 2.5 | 89 |
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| [References]
[1] Günther J, et al. BAY-069, a Novel (Trifluoromethyl)pyrimidinedione-Based BCAT1/2 Inhibitor and Chemical Probe. J Med Chem. 2022 Oct 19. DOI:10.1021/acs.jmedchem.2c00441 |
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