Art. -Nr.: HY-100490A

Rilmenidine hemifumarate

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Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na⁺/H⁺ antiport. Rilmenidine hemifumarate 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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Reinheit: 98.0%
CAS. Nr.: 207572-68-7
Formel: C₁₀H₁₆N_2O.1/2C₄H₄O₄
Molecular Weight:238.28

Speicherung:

-20°C, stored under nitrogen, away from moisture

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

Rilmenidine hemifumarate Chemical Structure

CAS. Nr.: 207572-68-7

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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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.

Chemical Information

CAS. Nr. 207572-68-7
Appearance Solid
Molecular Weight 238.28
Formel C₁₀H₁₆N_2O.1/2C₄H₄O₄
Color White to off-white
SMILES

O=C(O)/C=C/C(O)=O.C1(NC(C2CC2)C3CC3)=NCCO1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen, away from moisture

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

Lösungsmittel & Löslichkeit

In Vitro:

H₂O : ≥ 50 mg/mL (209.84 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.1967 mL

20.9837 mL

41.9674 mL

5 mM

0.8393 mL

4.1967 mL

8.3935 mL

10 mM

0.4197 mL

2.0984 mL

4.1967 mL

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 (stored under nitrogen, 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1 mg/mL (4.20 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 1 mg/mL (4.20 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1 mg/mL (4.20 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 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) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Reid JL. Rilmenidine: a clinical overview. Am J Hypertens. 2000;13(6 Pt 2):106S-111S. [Content Brief]

[2]. Srdic-Rajic T, et al. Rilmenidine suppresses proliferation and promotes apoptosis via the mitochondrial pathway in human leukemic K562 cells. Eur J Pharm Sci. 2016;81:172-180. [Content Brief]

[3]. Rose C, et al. Rilmenidine attenuates toxicity of polyglutamine expansions in a mouse model of Huntington's disease. Hum Mol Genet. 2010;19(11):2144-2153. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O	1 mM	4.1967 mL	20.9837 mL	41.9674 mL	104.9186 mL
	5 mM	0.8393 mL	4.1967 mL	8.3935 mL	20.9837 mL
	10 mM	0.4197 mL	2.0984 mL	4.1967 mL	10.4919 mL
	15 mM	0.2798 mL	1.3989 mL	2.7978 mL	6.9946 mL
	20 mM	0.2098 mL	1.0492 mL	2.0984 mL	5.2459 mL
	25 mM	0.1679 mL	0.8393 mL	1.6787 mL	4.1967 mL
	30 mM	0.1399 mL	0.6995 mL	1.3989 mL	3.4973 mL
	40 mM	0.1049 mL	0.5246 mL	1.0492 mL	2.6230 mL
	50 mM	0.0839 mL	0.4197 mL	0.8393 mL	2.0984 mL
	60 mM	0.0699 mL	0.3497 mL	0.6995 mL	1.7486 mL
	80 mM	0.0525 mL	0.2623 mL	0.5246 mL	1.3115 mL
	100 mM	0.0420 mL	0.2098 mL	0.4197 mL	1.0492 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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Rilmenidine hemifumarate

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Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Rilmenidine hemifumarate Related Classifications

HY-100490A Related Classifications