Rilmenidine

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。

Rilmenidine 

Rilmenidine 是一种新型的抗高血压药物和口服活性选择性 I1 咪唑啉受体 (I1 imidazoline receptor) 激动剂。Rilmenidine 是一种 α2 肾上腺素受体激动剂。Rilmenidine 诱导自噬 (autophagy)。Rilmenidine 可通过减少交感神经过度活跃而发挥中枢作用,并通过抑制 Na+/H+ 反向转运而在肾脏中发挥作用。Rilmenidine 可调节白血病细胞增殖,刺激促凋亡蛋白 Bax,从而诱导人白血病 K562 细胞线粒体通路的紊乱和凋亡。

Rilmenidine

Rilmenidine Chemical Structure

CAS No. : 54187-04-1

规格 是否有货
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250 mg   询价  
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Rilmenidine 的其他形式现货产品:

Rilmenidine hemifumarate

生物活性

Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].

体外研究
(In Vitro)

Rilmenidine provides antihypertensive efficacy comparable with that of diuretics, beta-blockers, calcium channel blockers, and angiotensin-converting enzyme (ACE) inhibitors[1].
Rilmenidine (25-100 μM; 24 hours) inhibits K562 cell proliferation[2].

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

Cell Viability Assay[2]

Cell Line: K562 cells
Concentration: 25, 50, 100 μM
Incubation Time: 24 hours
Result: Dose-dependently inhibited K562 colony formation.

体内研究
(In Vivo)

Rilmenidine-treated N171-82Q mice (i.p.; 4-times a week) displays significant improved forelimb grip strength and all limbs grip strength from 12 to 22 weeks of age[3].
Rilmenidine decreases levels of mutant huntingtin[3].

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

Clinical Trial

分子量

180.25

Formula

C10H16N2O

CAS 号

54187-04-1

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]. Reid JL. Rilmenidine: a clinical overview. Am J Hypertens. 2000;13(6 Pt 2):106S-111S.

    [2]. Srdic-Rajic T, et al. Rilmenidine suppresses proliferation and promotes apoptosis via the mitochondrial pathway in human leukemic K562 cells. Eur J Pharm Sci. 2016;81:172-180.

    [3]. Rose C, et al. Rilmenidine attenuates toxicity of polyglutamine expansions in a mouse model of Huntington’s disease. Hum Mol Genet. 2010;19(11):2144-2153.

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