# | Name | Compound Key | Action Type | Relation | Activity Value | Units | Assay ID | Assay Description | Comment | Assay | Assay Organism | |
---|---|---|---|---|---|---|---|---|---|---|---|---|
1. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Radiolabel recovery | = | 4.5 | % | ALA3508826 | % | ||||
2. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Radiolabel recovery | = | 4.04 | % | ALA3508825 | % | ||||
3. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Radiolabel recovery | = | 4 | % | ALA3508978 | VALUE = 93% of radioactivity was recovered in the excreta within 48h in the receiver rat | % | |||
4. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Radiolabel recovery | = | 0.6 | % | ALA3508977 | VALUE = 93% of radioactivity was recovered in the excreta within 48h in the receiver rat and the combined amount of radioactivity found in bile and urine (2.8% of the infused radioactivity) was absorbed from the duodenum and was available for enterohepatic circulation | % | |||
5. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Radiolabel recovery | = | 2.2 | % | ALA3508976 | VALUE = 93% of radioactivity was recovered in the excreta within 48h in the receiver rat and the combined amount of radioactivity found in bile and urine (2.8% of the infused radioactivity) was absorbed from the duodenum and was available for enterohepatic circulation | % | |||
6. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Radiolabel recovery | = | 26.6 | % | ALA3508975 | VALUE = 93% of radioactivity was recovered in the excreta within 48h in the receiver rat and the sum of radioactivity in GI tract and faeces (86.4%) represents unabsorbed test substance | % | |||
7. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Radiolabel recovery | = | 59.8 | % | ALA3508974 | VALUE = 93% of radioactivity was recovered in the excreta within 48h in the receiver rat and the sum of radioactivity in GI tract and faeces (86.4%) represents unabsorbed test substance | % | |||
8. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Radiolabel recovery | = | 4.6 | % | ALA3508973 | VALUE = 83% of radioactivity was recovered within 24h in the donor rat | % | |||
9. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Radiolabel recovery | = | 6.2 | % | ALA3508972 | VALUE = 83% of radioactivity was recovered within 24h in the donor rat | % | |||
10. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Radiolabel recovery | = | 70 | % | ALA3508971 | VALUE = 83% of radioactivity was recovered within 24h in the donor rat | % | |||
11. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Activity | 0 | ALA3508970 | OUTCOME = Observed, VALUE = CYP2D6 contributed to a minor extent on metabolism of aliskiren | Homo sapiens | |||||
12. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Activity | = | 99.6 | % | ALA3508969 | VALUE = CYP3A4/5 was contributing predominantly (99.6%) to the oxidative metabolism of aliskiren | % | Homo sapiens | ||
13. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Vmax | = | 1807.6 | pmol.min.mg-1 | ALA3508968 | pmol.min.mg-1 | ||||
14. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Km | = | 43.8 | uM | ALA3508967 | nM | ||||
15. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Fu unbound fraction | = | 51.4 | % | ALA3508892 | |||||
16. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Fu unbound fraction | = | 47.3 | % | ALA3508891 | |||||
17. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Fu unbound fraction | = | 49.8 | % | ALA3508890 | |||||
18. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Fu unbound fraction | = | 8.1 | % | ALA3508889 | |||||
19. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Fu unbound fraction | = | 42.5 | % | ALA3508888 | |||||
20. | ALA3508698 | [14C]Aliskiren hemifumarate, [14C]-SPP100 hemifumarate | Fu unbound fraction | = | 38.3 | % | ALA3508887 |