[CAS NO. 207572-68-7] Rilmenidine hemifumarate
PRODUCTS SPECIFICATIONS [207572-68-7]
DESCRIPTION [207572-68-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 238.28 |
| Molecular Formula | C10H16N2O.1/2C4H4O4 |
| SMILES | O=C(O)/C=C/C(O)=O.C1(NC(C2CC2)C3CC3)=NCCO1.[0.5] |
Summary
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 [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 (25-100 μM; 24 hours) inhibits K562 cell proliferation
[2]
.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00892892 | University of Erlangen-Nürnberg Medical School |
Chronic Kidney Disease|Hypertension
|
November 2009 | Phase 4 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Solvent & Solubility
H 2 O : 50 mg/mL ( 209.84 mM ; Need ultrasonic)
DMSO : 10 mg/mL ( 41.97 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 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 |
References
- [1] Reid JL. Rilmenidine: a clinical overview. Am J Hypertens. 2000;13(6 Pt 2):106S-111S.
- [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.
- [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.