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

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 .

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Rilmenidine phosphate Chemical Structure

Rilmenidine phosphate Chemical Structure

CAS No. : 85409-38-7

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5 mg USD 100 In-stock
10 mg USD 170 In-stock
25 mg USD 340 In-stock
50 mg USD 590 In-stock
100 mg USD 1050 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

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].

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

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[3].
Rilmenidine phosphate 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

278.24

Formula

C10H19N2O5P

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

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; 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 3.5940 mL 17.9701 mL 35.9402 mL
5 mM 0.7188 mL 3.5940 mL 7.1880 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: ≥98.0%

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). 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 / H2O 1 mM 3.5940 mL 17.9701 mL 35.9402 mL 89.8505 mL
5 mM 0.7188 mL 3.5940 mL 7.1880 mL 17.9701 mL
10 mM 0.3594 mL 1.7970 mL 3.5940 mL 8.9850 mL
15 mM 0.2396 mL 1.1980 mL 2.3960 mL 5.9900 mL
H2O 20 mM 0.1797 mL 0.8985 mL 1.7970 mL 4.4925 mL
25 mM 0.1438 mL 0.7188 mL 1.4376 mL 3.5940 mL
30 mM 0.1198 mL 0.5990 mL 1.1980 mL 2.9950 mL
40 mM 0.0899 mL 0.4493 mL 0.8985 mL 2.2463 mL
50 mM 0.0719 mL 0.3594 mL 0.7188 mL 1.7970 mL
60 mM 0.0599 mL 0.2995 mL 0.5990 mL 1.4975 mL
80 mM 0.0449 mL 0.2246 mL 0.4493 mL 1.1231 mL
100 mM 0.0359 mL 0.1797 mL 0.3594 mL 0.8985 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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Rilmenidine phosphate
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HY-100490B
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