| 产品描述: | 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 |
| 靶点: |
Imidazoline Receptor;Adrenergic Receptor;Apoptosis;Autophagy;Apoptosis; ImidazolineReceptor |
| 体外研究: |
Rilmenidine provides antihypertensive efficacy comparable with that of diuretics, beta-blockers, calcium channel blockers, and angiotensin-converting enzyme (ACE) inhibitors. Rilmenidine (25-100 μM; 24 hours) inhibits K562 cell proliferation. Cell Viability Assay Cell Line: K562 cells Concentration: 25, 50, 100 μM Incubation Time: 24 hours Result: Dose-dependently inhibited K562 colony formation. |
| 体内研究: |
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. Rilmenidine decreases levels of mutant huntingtin. |
| 参考文献: |
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. |
| 溶解性: |
Soluble in DMSO、H2O |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.098 ml |
10.492 ml |
20.983 ml |
| 5 mM |
0.42 ml |
2.098 ml |
4.197 ml |
| 10 mM |
0.21 ml |
1.049 ml |
2.098 ml |
| 50 mM |
0.042 ml |
0.21 ml |
0.42 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |