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

Rilmenidine phosphate 

Cat. No.: HY-100490B Purity: >98.0%
Handling Instructions

Rilmenidine phosphate, an antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate is also an alpha 2-adrenoceptor agonist. 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.

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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 antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate is also an alpha 2-adrenoceptor agonist. 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].

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 : 83.33 mg/mL (299.49 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
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

RilmenidineImidazoline ReceptorAdrenergic ReceptorApoptosisAutophagyBeta Receptorproliferation,antihypertensiveproapoptoticmitochondrialleukemicK562cellsInhibitorinhibitorinhibit

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Rilmenidine phosphate
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HY-100490B
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