1. Neuronal Signaling GPCR/G Protein Apoptosis Autophagy
  2. Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy
  3. Rilmenidine

Rilmenidine 是一种新型的抗高血压活性分子和口服活性选择性 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。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 Rilmenidine phosphateRilmenidine hemifumarate 通常具有更好的水溶性和稳定性。

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Rilmenidine Chemical Structure

Rilmenidine Chemical Structure

CAS No. : 54187-04-1

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Rilmenidine 的其他形式现货产品:

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查看 Adrenergic Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE 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].

MCE 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
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.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Rilmenidine
目录号:
HY-100490
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