标签归档：veledimex

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

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Veledimex (S enantiomer) (Synonyms: INXN-1001 (S enantiomer); RG-115932 (S enantiomer)) 纯度: 99.52%

Veledimex S enantiomer (INXN-1001 S enantiomer) 是 Veledimex 的 S 型异构体。Veledimex 是一种具有口服活性的专有基因研究启动系统的激活剂配体，也是 CYP3A4/5 的温和抑制剂配体。

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

Veledimex (S enantiomer) Chemical Structure

CAS No. : 1093131-03-3

规格 价格 是否有货 数量
5 mg ￥7500 In-stock
10 mg ￥11000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Veledimex (S enantiomer) 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

Veledimex S enantiomer (INXN-1001 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[1].

体内研究
(In Vivo)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

438.60

Formula

C27H38N2O3
CAS 号

1093131-03-3
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
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [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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Veledimex racemate(Synonyms: INXN-1001 racemate; RG-115932 racemate)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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

Veledimex racemate (INXN-1001 racemate) 是 Veledimex 的外消旋体。Veledimex 是 RheoSwitch 系统中有口服活性的小分子激活剂配体。

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

Veledimex racemate Chemical Structure

CAS No. : 755013-59-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

Veledimex racemate (INXN-1001 racemate) is the racemate of veledimex. Veledimex is an orally available, small-molecule activator ligand for the RheoSwitch Therapeutic System[1].

体外研究
(In Vitro)

Interleukin 12 (IL-12) is a pro-inflammatory cytokine critical for stimulating anti-cancer immune responses. Ad-RTS-IL-12 is the adenovirusvector engineered to express hIL-12. Veledimex is an orally active small-molecule diacylhydrazine and controls the expression of the target gene. The amount of gene product produced by the system and the duration of the effect are dependent on veledimex dose level and duration of dosing[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Veledimex, combined with Ad-RTS-hIL-12, is in phase I/II clinical trials for the treatment of melanoma and breast cancer. Intratumoral administration of Ad-RTS-mIL-12 along with oral administration of veledimex elicits dose-dependent antitumor effects in murine melanoma, breast cancer, and glioma models, 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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

438.60

Formula

C27H38N2O3
CAS 号

755013-59-3
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
In solvent -80°C 6 months
-20°C 1 month
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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

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

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Veledimex (Synonyms: INXN-1001; RG-115932) 纯度: 99.19%

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)。

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

Veledimex Chemical Structure

CAS No. : 1093130-72-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3520 In-stock
5 mg ￥3200 In-stock
10 mg ￥5400 In-stock
50 mg ￥17000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Veledimex 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • CNS-Penetrant Compound Library
  • Drug Repurposing Compound Library
  • Orally Active Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library
  • Rare Diseases Drug Library

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[1][2].

IC50 & Target

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[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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

438.60

Formula

C27H38N2O3
CAS 号

1093130-72-3
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (57.00 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2800 mL 11.3999 mL 22.7998 mL
5 mM 0.4560 mL 2.2800 mL 4.5600 mL
10 mM 0.2280 mL 1.1400 mL 2.2800 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.70 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务