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

Rilmenidine phosphate 

目录号: HY-100490B 纯度: >98.0%
产品使用指南

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。

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Rilmenidine phosphate Chemical Structure

Rilmenidine phosphate Chemical Structure

CAS No. : 85409-38-7

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Description

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][4].

In Vitro

Rilmenidine phosphate (25-100 μM; 24 hours) inhibits K562 cell proliferation[2]. Rilmenidine provides antihypertensive efficacy comparable with that of diuretics, beta-blockers, calcium channel blockers, and angiotensin-converting enzyme (ACE) inhibitors[3].

Cell Proliferation Assay[2]

Cell Line: K562 cells
Concentration: 25, 50, 100 μM
Incubation Time: 24 hours
Result: Dose-dependently inhibited K562 colony formation.
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[4].
Rilmenidine phosphate decreases levels of mutant huntingtin[4].

Molecular Weight

278.24

Formula

C₁₀H₁₉N₂O₅P

CAS No.

85409-38-7

SMILES

O=P(O)(O)O.C1(NC(C2CC2)C3CC3)=NCCO1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 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。 -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。

References
  • 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)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

RilmenidineImidazoline ReceptorAdrenergic ReceptorApoptosisAutophagyBeta Receptorproliferation,antihypertensiveproapoptoticmitochondrialleukemicK562cellsInhibitorinhibitorinhibit

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Rilmenidine phosphate
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