Veledimex (S enantiomer)
Names
[ CAS No. ]:
1093131-03-3
[ Name ]:
Veledimex (S enantiomer)
Biological Activity
[Description]:
Veledimex S enantiomer is the S enantiomer of veledimex. Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5.
[Related Catalog]:
[In Vivo]
Veledimex generally has moderate to low oral bioavailability after a single oral administration in mice and monkeys (∼56% in mice and up to 17.4% in cynomolgus monkeys) with mostly low plasma clearance (1399 and 1170 mL/h per kilogram in mice and monkeys, respectively), high volume of distribution (20271 and 9180 mL/h per kilogram in mice and monkeys, respectively), and long terminal half-lives (∼10 hours in mice and ∼30 hours in monkeys) after intravenous administration[1]. Ad-RTS-mIL-12 + veledimex have demonstrated a dose-related increase in tumor IL-12 mRNA and IL-12 protein expression. Discontinuation of veledimex resulted in a return to baseline IL-12 mRNA and protein expression in numerous syngeneic mouse tumor models. Veledimex crosses the blood-brain-barrier in both naive and orthotopic GL-261 mice with increased brain tissue level of ∼6 fold observed in tumor bearing vs. normal mice. Ad-RTS-mIL-12 + veledimex demonstrate a dose-related increase in survival without significant adverse events[2].
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Molecular Formula ]:
C27H38N2O3
[ Molecular Weight ]:
438.6
[ Storage condition ]:
2-8℃