Veledimex (INXN-1001)

Veledimex (INXN-1001) (INXN-1001) 是昆虫蜕皮激素蜕皮激素的合成类似物，是专有基因治疗启动子系统的口服活性激活剂配体。

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库存: 现货

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价格

促销价

数量
1mg

￥1612.00

1290.00

- +
5mg

￥3737.00

2990.00

- +
10mg

￥6412.00

5130.00

- +
25mg

￥12712.00

10170.00

- +
50mg

￥20125.00

16100.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajce47824
CAS: 1093130-72-3
别名: INXN-1001; RG-115932
分子式: C27H38N2O3
分子量: 438.6
纯度: >98%
溶解度: DMSO : 25 mg/mL (57.00 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

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.