DPC-423 is a factor Xa inhibitor potentially for the treatment of thrombosis. In vivo and in vitro studies with the synthetic oxime intermediate from DPC-423 showed an adduct identical to the one isolated from the bile of rats dosed with DPC-423. This supported the intermediacy of an aldoxime as a precursor to the GSH adducts. It is postulated that the benzylamine moiety of DPC-423 (and its analogues) is oxidized to a hydroxylamine, which is subsequently converted to a nitroso intermediate. Subsequent rearrangement of the nitroso leads to an aldoxime which in turn is metabolized by P450 to a reactive intermediate. The formation of oxime from DPC-423 (and its analogues) was found to be mediated by rat CYP 3A1/2, which were also responsible for converting the oxime to the GSH trappable reactive intermediate.
MedKoo Cat#: 528203
Name: DPC-423 HCl
CAS#: 292135-59-2 (HCl)
Chemical Formula: C25H21ClF4N4O3S
Exact Mass: 0.0000
Molecular Weight: 568.97
Elemental Analysis: C, 52.78; H, 3.72; Cl, 6.23; F, 13.36; N, 9.85; O, 8.44; S, 5.63
The following data is based on the product molecular weight 568.97 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
