. 2019 Feb 21;40(8):1106–1118. doi: 10.1038/s41401-019-0218-8

Table 1.

Kinetic parameters (mean ± SD of 3 rats) for formations of β-oxidative and reductive metabolites on acyl side chain of pyragrel (Pyr), ozagrel (Oza) and cinnamic acid (Cin) in primary hepatocytes (Hep), isolated hepatic mitochondria (Mit) and microsomes (Mic) of rats

Compounds	System	Reaction	Cofactor	K_m (μM)	V_max (pmol min⁻¹ mg⁻¹ or pmol min⁻¹ 10⁻⁵ cells)	N	^aCL_int_{, in vitro} (μL min⁻¹ mg⁻¹ or μL min⁻¹ 10⁻⁵ cells)	^bCL_{int, in vivo} (mL min⁻¹ kg⁻¹)	^cCL_H (mL min⁻¹ kg⁻¹)
Pyr	Hep	Oxidation	-	37.65 ± 6.96	12.38 ± 1.07	-	0.33 ± 0.04	6.70 ± 0.83	3.95
	Hep	Reduction	-	139.29 ± 11.93	43.08 ± 1.06	-	0.31 ± 0.02	6.23 ± 0.36
	Mit	Oxidation	NAD⁺	145.55 ± 10.42	275.15 ± 40.23	-	1.90 ± 0.35	3.04 ± 0.56	3.15
	Mit	Reduction	NADH	100.29 ± 9.15	81.98 ± 6.29	-	0.82 ± 0.02	1.31 ± 0.02
	Mit	Reduction	NADPH	152.85 ± 44.68	321.73 ± 27.73	-	2.25 ± 0.80	3.06 ± 1.28
	Mic	Reduction	NADPH	534.81 ± 140.17	805.07 ± 150.23	-	1.53 ± 0.14	2.75 ± 0.26
Oza	Hep	Oxidation	-	78.21 ± 3.09	64.71 ± 1.69	-	0.83 ± 0.01	16.62 ± 0.23	5.03
	Hep	Reduction	-	188.10 ± 43.94	186.98 ± 28.13	1.51 ± 0.33	0.55 ± 0.02	11.07 ± 0.57
	Mit	Oxidation	NAD⁺	1119.61 ± 281.72	647.04 ± 25.68	-	0.61 ± 0.18	0.97 ± 0.28	1.32
	Mit	Reduction	NADH	2386.90 ± 838.21	674.45 ± 139.69	1.31 ± 0.20	0.18 ± 0.01	0.28 ± 0.02
	Mit	Reduction	NADPH	203.57 ± 53.07	731.56 ± 29.51	1.31 ± 0.09	2.19 ± 0.58	3.51 ± 0.93
	Mic	Reduction	NADPH	1889.86 ± 297.76	2078.98 ± 222.47	-	1.11 ± 0.06	1.99 ± 0.12
Cin	Hep	Oxidation	-	0.77 ± 0.12	18.02 ± 1.19	-	23.56 ± 1.91	473.13 ± 959.40	39.71
	Hep	Reduction	-	28.21 ± 7.24	39.68 ± 4.34	-	1.44 ± 0.22	28.98 ± 4.46
	Mit	Oxidation	NAD⁺	2.98 ± 0.15	577.87 ± 20.72	-	194.57 ± 16.33	311.31 ± 26.12	42.14
	Mit	Reduction	NADH	6.79 ± 0.98	144.03 ± 7.97	-	21.48 ± 2.89	34.36 ± 4.62
	Mit	Reduction	NADPH	5.89 ± 0.59	353.78 ± 57.78	-	60.26 ± 10.47	96.42 ± 16.75
	Mic	Reduction	NADPH	4.41 ± 0.09	464.45 ± 7.59	-	105.39 ± 2.41	189.71 ± 4.35

K_m, Michaelis constant, V_max the maximum reaction velocity, N the Hill coefficient

^aCL_{int, in vitro} (μL min⁻¹ mg⁻¹ or μL min⁻¹ 10⁻⁵ cells) was defined as V_max/K_m or V_max × (N−1)/(K_m × N × (N−1)^1/N).

^bCL_{int, in vivo} (mL min⁻¹ kg⁻¹) was estimated by CL_{int, in vitro} × SF, where SF was the product of protein yield (40 mg mitochondrial protein/g liver [26] or 45 mg microsomal protein/g liver [27]) or hepatocyte yield (5.02 × 10⁷ cells/g liver) [23] and the liver weight per kilogram of body weight (40 g/kg) [23]

^cCL_H (mL min⁻¹kg⁻¹) was predicted from the well-stirred model