Table 6

Metabolites of Org 30659 present in cell media from incubations with rat and human hepatocytes

Metabolites
Rat Cell MediumHuman Liver 4 Cell MediumHuman Liver 5 Cell Medium
H1, H2, H3, H4,H5, H6, H7, H9,H10, H11,6-a H12,H15,6-a H17,6-a H20,H21, H23, H24,H26 H4, H6,H8, H10, H11, H13,6-a H14, H15, H16, H18,  H19, H22, Org 30659,6-a H24,H25, H26 H6, H8,H13,6-a H21, Org 30659,6-a H24
  • The putative structures of the metabolites present in rat and human hepatocytes are as follows: H13, 6β-OH metabolite of Org 30659; H15, A-ring-opened 2-OH,4-carboxylic acid,5α-H metabolite of Org 30659; H17, A-ring-opened 2-OH,4-carboxylic acid,5α-H,15β-OH,Δ16,17-ethinyl metabolite of Org 30659; H18, 15β,16β-epoxide metabolite of Org 30659; H19, O-glucuronide of the 3α-OH,5α-H metabolite of Org 30659; H20, 3α-OSO3H,5α-H metabolite of Org 30659; H21, 3α-OSO3H,5α-H,15β-OH,Δ16,17-ethinyl metabolite of Org 30659; H24, 3β-OH,5α-H metabolite of Org 30659 and/or 5α-H metabolite of Org 30659; H26, 3α-OH,5α-H metabolite of Org 30659. All other metabolites were not previously identified.

  • 6-a Major compound after 3 hr of incubation.