Rilmenidine Phosphate

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

85409-38-7

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。

生物活性

Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selectiveI1imidazoline receptoragonist. Rilmenidine phosphate is analpha 2-adrenoceptoragonist. Rilmenidine phosphate inducesautophagy. 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 proteinBaxthus inducing the perturbation of the mitochondrial pathway andapoptosisin 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].

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].

Clinical Trial

分子量

278.24

性状

Solid

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℃)

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。