Rilmenidine phosphate

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Rilmenidine phosphate 

Rilmenidine phosphate 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 phosphate 也是一种 α2 肾上腺素受体激动剂。Rilmenidine phosphate 诱导自噬 (autophagy)。Rilmenidine phosphate 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 phosphate 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 phosphate

Rilmenidine phosphate Chemical Structure

CAS No. : 85409-38-7

规格 价格 是否有货
5 mg ￥1800 询问价格 & 货期
10 mg ￥2900 询问价格 & 货期
25 mg ￥5800 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate 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 phosphate (25-100 μM; 24 hours) inhibits K562 cell proliferation[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.

Cell Proliferation 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 phosphate-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 phosphate decreases levels of mutant huntingtin[3].

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

278.24

Formula

C10H19N2O5P
CAS 号

85409-38-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

H2O : 62.5 mg/mL (224.63 mM; Need ultrasonic)

DMSO : 5 mg/mL (17.97 mM; ultrasonic and warming and heat to 80°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5940 mL 17.9701 mL 35.9402 mL
5 mM 0.7188 mL 3.5940 mL 7.1880 mL
10 mM 0.3594 mL 1.7970 mL 3.5940 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 (sealed storage, away from moisture)。-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。
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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