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.
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- Pureté: 99.9%
- CAS No.: 54187-04-1
- Formule: C10H16N2O
- Masse moléculaire:180.25
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Stockage:
-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]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | IC50 |
65 μM
Compound: ChEMBLID-289480
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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
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[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.
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Cell Line:K562 cells
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Concentration:25, 50, 100 μM
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Incubation Time:24 hours
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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
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 54187-04-1
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Appearance Solid
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Masse moléculaire 180.25
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Formule C10H16N2O
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Color White to off-white
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SMILES
C1(NC(C2CC2)C3CC3)=NCCO1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-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)
Solvant et solubilité
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)
Pureté et documentation
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Fiche technique (275 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
[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
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