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Veledimex S enantiomer(INXN-1001 S enantiome)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Veledimex S enantiomer(INXN-1001 S enantiome)图片
CAS NO:1093131-03-3
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议
10mg电议

产品介绍
Veledimex S 对映体 (INXN-1001 S enantiomer) 是 veledimex 的 S 对映体。 Veledimex 是专有基因治疗启动子系统的口服激活剂配体，也是 CYP3A4/5 的中度抑制剂和底物。
Cas No.1093131-03-3
别名INXN-1001 (S enantiomer); RG-115932 (S enantiomer)
Canonical SMILESO=C(NN(C(C1=CC(C)=CC(C)=C1)=O)[C@H](C(C)(C)C)CCC)C2=CC=CC(OC)=C2CC
分子式C27H38N2O3
分子量438.6
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.