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

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.

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Rilmenidine

Rilmenidine Chemical Structure

CAS No. : 54187-04-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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].

Cellular Effect
Cell Line Type Value Description References
K562 IC50
65 μM
Compound: ChEMBLID-289480
Antiproliferative activity against human K562 cells assessed as inhibition of cell survival after 48 hrs by MTT assay
Antiproliferative activity against human K562 cells assessed as inhibition of cell survival after 48 hrs by MTT assay
[PMID: 27265687]
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].

MedChemExpress (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.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

180.25

Formula

C10H16N2O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C1(NC(C2CC2)C3CC3)=NCCO1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (554.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.5479 mL 27.7393 mL 55.4785 mL
5 mM 1.1096 mL 5.5479 mL 11.0957 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.90%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 5.5479 mL 27.7393 mL 55.4785 mL 138.6963 mL
5 mM 1.1096 mL 5.5479 mL 11.0957 mL 27.7393 mL
10 mM 0.5548 mL 2.7739 mL 5.5479 mL 13.8696 mL
15 mM 0.3699 mL 1.8493 mL 3.6986 mL 9.2464 mL
20 mM 0.2774 mL 1.3870 mL 2.7739 mL 6.9348 mL
25 mM 0.2219 mL 1.1096 mL 2.2191 mL 5.5479 mL
30 mM 0.1849 mL 0.9246 mL 1.8493 mL 4.6232 mL
40 mM 0.1387 mL 0.6935 mL 1.3870 mL 3.4674 mL
50 mM 0.1110 mL 0.5548 mL 1.1096 mL 2.7739 mL
60 mM 0.0925 mL 0.4623 mL 0.9246 mL 2.3116 mL
80 mM 0.0693 mL 0.3467 mL 0.6935 mL 1.7337 mL
100 mM 0.0555 mL 0.2774 mL 0.5548 mL 1.3870 mL
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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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Product Name:
Rilmenidine
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HY-100490
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