RR-11a

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。

RR-11a 

RR-11a是人工合成的天冬酰胺酰内肽酶 Legumain 抑制剂 (IC50=31-55 nM)。RR-11a 可用于癌症和急性心肌梗死 (AMI) 的研究。

RR-11a

RR-11a Chemical Structure

CAS No. : 1361390-56-8

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生物活性

RR-11a is a synthetic enzyme inhibitor of Legumain (IC50=31-55 nM). RR-11a can be used for the research of cancer and acute myocardial infarction (AMI)[1][2][3].

IC50 & Target[2]

Legumain

31-55 nM (IC50)

体外研究
(In Vitro)

Legumain-targeted RR-11a-coupled nanoparticles reveal high ligand-receptor affinity, enhance solid-tumor penetration and uptake by tumor cells[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)

Treatment of tumor-bearing mice with RR-11a-coupled NPs encapsulating doxorubicin results in improved tumor selectivity and drug sensitivity, leading to complete inhibition of tumor growth[1].
RR-11a (20 mg/kg; daily i.p. for 30 days) improves cardiac function, decreases cardiac rupture rate, and attenuates left chamber dilation and wall thinning post-AMI in mice[3].

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

分子量

560.51

Formula

C24H28N6O10

CAS 号

1361390-56-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Liao D, et al. Synthetic enzyme inhibitor: a novel targeting ligand for nanotherapeutic drug delivery inhibiting tumor growth without systemic toxicity. Nanomedicine. 2011 Dec;7(6):665-73.

    [2]. Ralph A, et al. Nanoparticle-based tumor-targeted drug delivery. Patent: CA2809617C

    [3]. Yang H, et al. Legumain is a predictor of all-cause mortality and potential therapeutic target in acute myocardial infarction. Cell Death Dis. 2020;11(11):1014. Published 2020 Nov 26.

Animal Administration
[1]

Mice[1]

Mice bearing 4T1 orthothopic tumors of approximately 500 mm3 are injected once intravenously with RR-11a+ or RR-11a-nanoparticles labeled with rhodamine B. Alternatively, mice are injected intravenously 3 times at 48-hour intervals with RDZ-218, NP-DOX, free DOX, or saline. Twenty-four hours after the final treatment, animals are sacrificed and spleen, kidney, lungs, liver, heart and tumor are collected, frozen in OCT compound, immediately sectioned and imaged by fluorescence microscopy[1].

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

参考文献
  • [1]. Liao D, et al. Synthetic enzyme inhibitor: a novel targeting ligand for nanotherapeutic drug delivery inhibiting tumor growth without systemic toxicity. Nanomedicine. 2011 Dec;7(6):665-73.

    [2]. Ralph A, et al. Nanoparticle-based tumor-targeted drug delivery. Patent: CA2809617C

    [3]. Yang H, et al. Legumain is a predictor of all-cause mortality and potential therapeutic target in acute myocardial infarction. Cell Death Dis. 2020;11(11):1014. Published 2020 Nov 26.

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