Cat. No.: HY-100490

Rilmenidine

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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.

For research use only. We do not sell to patients.

Purity: 99.9%
CAS No.: 54187-04-1
Formula: C₁₀H₁₆N₂O
Molecular Weight:180.25

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)

Rilmenidine Chemical Structure

CAS No.: 54187-04-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Adrenergic Receptor Isoforms :

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 54187-04-1
Appearance Solid
Molecular Weight 180.25
Formula C₁₀H₁₆N₂O
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)

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

5.5479 mL

27.7393 mL

55.4785 mL

5 mM

1.1096 mL

5.5479 mL

11.0957 mL

10 mM

0.5548 mL

2.7739 mL

5.5479 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 (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

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

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Molecular Weight Molecular Weight

Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)

References

[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
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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Rilmenidine

Apoptosis Compound Library

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Autophagy Compound Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

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Anti-Obesity Compound Library

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FDA-Approved Anticancer Drug Library

Human Metabolite Library

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Antihypertensive Compound Library

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Highly Selective Activators Library

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MCE Bioactive Compound Library

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Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

All Adrenergic Receptor Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Rilmenidine Related Classifications

HY-100490 Related Classifications