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Veledimex racemate

产品编号 T13293 CAS 755013-59-3

别名: RG-115932 racemate, INXN-1001 racemate

Veledimex racemate, the racemic form of veledimex, is an orally available, small-molecule ligand that activates the RheoSwitch Therapeutic System.

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Veledimex racemate, CAS 755013-59-3

规格	价格/CNY	货期
25 mg	￥ 13,900	8-10周
50 mg	￥ 18,300	8-10周
100 mg	￥ 23,500	8-10周

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其他形式的 Veledimex racemate:

Veledimex (S enantiomer)
询价
Veledimex
询价

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Veledimex racemate, the racemic form of veledimex, is an orally available, small-molecule ligand that activates the RheoSwitch Therapeutic System.
体外活性	Interleukin 12 (IL-12) is a pro-inflammatory cytokine critical for stimulating anti-cancer immune responses. Ad-RTS-IL-12 is an adenovirus vector engineered to express hIL-12. Veledimex is an orally active small molecule diacylhydrazine, which can control the expression of target genes. The amount of gene product produced by the system and the duration of action depend on the dose level of veledimex and the time of administration.
体内活性	In murine melanoma, breast cancer, and glioma models, Intratumoral administration of Ad-RTS-mIL-12 along with oral administration of veledimex elicits dose-dependent antitumor effects , which correlates with increased plasma exposure of veledimex. The increase in tumor veledimex levels in combination with Ad-RTS-mIL-12 results in a dose-related increase in the IL-12 mRNA (switch on) leading to dose-related increases in IL-12p70 in the tumor with minimal increase in serum IL-12. The increase in tumor IL-12 correlates with an increase in tumor CD8+ cytotoxic T cells and a concomitant decrease in regulatory T cells in the tumor microenvironment, which leads to Ad-RTS-mIL-12 + veledimex–elicited dose-related decreases in tumor growth rate with no significant change in body weight in both breast and melanoma syngeneic mouse models. Veledimex 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.

别名	RG-115932 racemate, INXN-1001 racemate
分子量	438.6
分子式	C27H38N2O3
CAS No.	755013-59-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Cai H, et al. Plasma Pharmacokinetics of Veledimex, a Small-Molecule Activator Ligand for a Proprietary GeneTherapy Promoter System, in Healthy Subjects. Clin Pharmacol Drug Dev. 2017 May;6(3):246-257.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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