Table 2.

IC₅₀ or EC₅₀ values of CsA, ALV, and different SMCypIs derivatives from C31 for inhibition of CypD PPIase activity in an enzyme assay, and for mitochondrial swelling and calcium retention capacity in isolated mouse liver mitochondria

Compound	CypD PPIase activity IC50 (μM)	Mitochondrial swelling IC50 (μM)	Calcium retention capacity EC50 (μM)
CsA	0.02 ± 0.003	0.05 ± 0.01	0.23 ± 0.02
ALV	0.03 ± 0.005	0.05 ± 0.02	0.08 ± 0.02
C31	0.20 ± 0.10	1.30 ± 0.05	9.09 ± 0.21
C183	1.03 ± 0.13	2.56 ± 0.02	10.21 ± 0.06
C144	0.64 ± 0.15	11.57 ± 0.01	11.76 ± 0.01
C105	0.57 ± 0.12	0.69 ± 0.05	2.37 ± 0.11
C110	0.11 ± 0.01	0.37 ± 0.006	2.83 ± 0.09
C105SR	0.005 ± 0.001	0.009 ± 0.001	0.05 ± 0.02
C110SR	0.008 ± 0.002	0.04 ± 0.005	0.14 ± 0.02

ALV, alisporivir; CsA, cyclosporin A; CypD, cyclophilin D; PPIase, peptidyl-prolyl cis-trans isomerase.