Veledimex S enantiomer (INXN-1001 S enantiome) (Synonyms: INXN-1001 (S enantiomer); RG-115932 (S enantiomer)) |
カタログ番号GC30705 |
Veledimex S エナンチオマー (INXN-1001 S エナンチオマー) は、veledimex の S エナンチオマーです。 Veledimex は、独自の遺伝子治療プロモーター システムの経口活性化リガンドであり、CYP3A4/5 の中程度の阻害剤および基質です。
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Cas No.: 1093131-03-3
Sample solution is provided at 25 µL, 10mM.
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.
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].
[1]. Cai H, et al. Plasma Pharmacokinetics of Veledimex, a Small-Molecule Activator Ligand for a Proprietary Gene Therapy Promoter System, in Healthy Subjects. Clin Pharmacol Drug Dev. 2017 May;6(3):246-257. [2]. John A. Barrett, INTRATUMORAL REGULATED EXPRESSION OF IL-12 AS A GENE THERAPY APPROACH TO TREATMENT OF GLIOMA. Neuro Oncol. 2015 Nov; 17(Suppl 5): v113.
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