Synthesis and In Vitro AMPK Activation of Cycloalkyl/Alkarylbiguanides with Robust In Vivo Antihyperglycemic Action

Table 2

Toxicity profiles predicted for compounds 4–6, metformin, and phenformin.

Compd.	LD50 (mg/kg)				Probability of inhibition; (IC50 or  μM)
	Mouse		Rat		CYP450 isoform			hERG
	i.p.	p.o.	i.p.	p.o.	3A4	2D6	1A2
4	400	510	260	850	0.01	0.06	0.01	0.02
5	190	640	130	750	0.01	0.04	0.01	0.03
6	170	710	240	850	0.01	0.10	0.03	0.05
Metformin	247	810	220	960	0.01	0.02	0.01	0.01
Phenformin	160	720	240	890	0.02	0.12	0.04	0.07