Veledimex|1093130-72-3|(INXN-1001; RG-115932)-陌孚医药/Medlife

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Veledimex (Synonyms: INXN-1001; RG-115932)

目录号: PL04674 纯度: ≥98%

Veledimex (INXN-1001) 是昆虫蜕皮激素蜕皮激素的合成类似物，是一种具有口服活性的用于专有的基因治疗启动子系统的激活配体。Veledimex 可利用蜕皮激素受体 (EcR) 诱导基因调控系统RheoSwitch治疗系统 (RTS) 激活某些基因。Veledimex 可透过在原位 GL-261 小鼠和食蟹猴的血脑屏障 (BBB)。

CAS No. :1093130-72-3

商品编号	规格	价格	会员价
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PL04674-10mg	10mg	¥8679.00	请登录
PL04674-50mg	50mg	¥27323.00	请登录
PL04674-100mg	100mg	询价	询价
PL04674-200mg	200mg	询价	询价
PL04674-10mM*1mLinDMSO	10mM*1mLinDMSO	¥5657.00	请登录

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中文名称	Veledimex
中文别名	N'-(3,5-dimethylbenzoyl)-N'-[(3R)-2,2-dimethylhexan-3-yl]-2-ethyl-3-methoxybenzohydrazide;Veledimex
英文名称	Veledimex
英文别名	Veledimex;ASU841TV0X;N'-(3,5-dimethylbenzoyl)-N'-[(3R)-2,2-dimethylhexan-3-yl]-2-ethyl-3-methoxybenzohydrazide;Veledimex [USAN:INN];Veledimex (USAN/INN);DB12170;D10678;Q27274109;(r)-3,5-dimethyl-benzoic acid n-(1-tert-butyl-butyl)-n'-(2-ethyl-3-methoxy-benzoyl)-hydrazide
Cas No.	1093130-72-3
分子式	C₂₇H₃₈N₂O₃
分子量	438.60
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

生物活性

Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys.

性状

Solid

IC50 & Target[1][2]

IL-12

体内研究(In Vivo)

Veledimex (INXN-1001) 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. 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 tumo

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Barrett JA, et al. Regulated intratumoral expression of IL-12 using a RheoSwitch Therapeutic System? (RTS?) gene switch as gene therapy for the treatment of glioma. Cancer Gene Ther. 2018;25(5-6):106-116.
[2]. Chiocca EA, et al. Regulatable interleukin-12 gene therapy in patients with recurrent high-grade glioma: Results of a phase 1 trial. Sci Transl Med. 2019;11(505):eaaw5680.

溶解度数据	In Vitro: DMSO : 25 mg/mL (57.00 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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