Assay
|
Aldosterone synthase (CYP11B2) IC50, nmol/L
|
11β-hydroxylase (CYP11B1) IC50, nmol/L
|
Selectivity ratioa(CYP11B2:CYP11B1)
|
---|
Recombinant human enzyme
|
0.7 ± 0.01 (6)
|
2.5 ± 0.1 (4)
|
3.6
|
Recombinant rat enzyme
|
160 ± 9 (3)
|
410 ± 5 (3)
|
2.6
|
Rat adrenal homogenate
|
802 (2)
|
3045 (2)
|
3.8
|
Monkey adrenal homogenate
|
12 ± 1 (6)
|
62 ± 5 (6)
|
5.2
|
- Table shows selectivity ratios for LCI699 for inhibition of aldosterone synthase (CYP11B2) over 11β-hydroxylase (CYP11B1). All values are mean ± SEM (n) except for rat adrenal homogenate where only mean values from two experiments are presented.
-
aSelectivity ratio is defined as the ratio of IC50 values obtained in the CYP11B2 and CYP11B1 assays.
- CYP, cytochrome P450; IC50, half maximal inhibitory concentration.