Rilmenidine
Based on 1 Customer Validation
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.9%
- No. CAS: 54187-04-1
- Fòrmula: C10H16N2O
- Peso molecular:180.25
-
Almacenamiento:
-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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
Anti-Cardiovascular Disease Compound Library
HY-L046
-
Orally Active Compound Library
HY-L061
-
Neurotransmitter Receptor Compound Library
HY-L062
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Anti-Obesity Compound Library
HY-L087
-
Rare Diseases Drug Library
HY-L102
-
Antidepressant Compound Library
HY-L108
-
EMA-Approved Drug Library
HY-L116
-
FDA-Approved Anticancer Drug Library
HY-L122
-
Human Metabolite Library
HY-L123
-
Off-patent Drug Library
HY-L141
-
Antihypertensive Compound Library
HY-L145
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Activators Library
HY-L159
-
Cell Death Library
HY-L162
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
Bioactive Compound Library
HY-L001
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Lactylation Compound Library
HY-L249
-
Apoptosis Compound Library
HY-L003
-
GPCR/G Protein Compound Library
HY-L006
-
Neuronal Signaling Compound Library
HY-L013
-
FDA-Approved Drug Library
HY-L022
-
Anti-Cancer Compound Library
HY-L025
-
Autophagy Compound Library
HY-L029
-
Drug Repurposing Compound Library
HY-L035
Ver todos los productos específicos de isoformas Adrenergic Receptor
More
Actividad biológica
|
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] |
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 Line:K562 cells
-
Concentration:25, 50, 100 μM
-
Incubation Time:24 hours
-
Result:Dose-dependently inhibited K562 colony formation.
Rilmenidine decreases levels of mutant huntingtin[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 54187-04-1
-
Appearance Solid
-
Peso molecular 180.25
-
Fòrmula C10H16N2O
-
Color White to off-white
-
SMILES
C1(NC(C2CC2)C3CC3)=NCCO1
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
-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)
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
-
Ficha de datos (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)
-
Instrucciones de manejo (2659 KB)
Referencias
[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]
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 |
Rilmenidine Related Classifications
HY-100490 Related Classifications
Powered by Bioz