Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Rilmenidine Phosphate, the water soluble form of Rilmenidine, is a potent and selective imidazoline receptor agonist used for the treatment of hypertension. In Hep G2 cells treated with 0.5 mM oleic acid for 6 hours and 1μm Rilmenidine for 30 minutes, the oleic acid-induced lipid accumulation decreases. Stimulation of imidazoline I-1 receptor by Rilmenidine activated P38 to induce the expression of FXR. Mice fed with HFD (high fat diet) had improved hepatic steatosis following the administration of Rilmenidien through the activation of imidazoline I-1 receptor.
ln Vitro |
The antihypertensive efficacy of rilmenidine is on par with that of ACE inhibitors, beta-blockers, calcium channel blockers, and diuretics[1]. K562 cells are inhibited from proliferating for 24 hours at 25–100 μM rimenidine phosphate[2].
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ln Vivo |
From 12 to 22 weeks of age, N171-82Q mice (ip; four times per week) treated with rimedinidine phosphate exhibit noticeably enhanced forelimb and all limb grip strength[3]. Huntingtin mutations are reduced by rilmenidine phosphate[3].
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Cell Assay |
Cell Proliferation Assay[2]
Cell Types: K562 cells Tested Concentrations: 25, 50, 100 μM Incubation Duration: 24 hrs (hours) Experimental Results: Dose-dependently inhibited K562 colony formation. |
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Animal Protocol |
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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. |
Molecular Formula |
C10H19N2O5P
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Molecular Weight |
278.24
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CAS # |
85409-38-7
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Related CAS # |
Rilmenidine;54187-04-1
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C1CC1C(C2CC2)NC3=NCCO3.OP(=O)(O)O
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.5940 mL | 17.9701 mL | 35.9402 mL | |
5 mM | 0.7188 mL | 3.5940 mL | 7.1880 mL | |
10 mM | 0.3594 mL | 1.7970 mL | 3.5940 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT00892892 | WITHDRAWN | Drug:Rilmenidine Drug:Nitrendipine |
Chronic Kidney Disease Hypertension |
University of Erlangen-Nürnberg Medical School |
2009-11 | Phase 4 |
NCT02539810 | TERMINATED | Device:Renal artery Angioplasty plus stenting. Drug:Anti hypertensive, statin and antiplatelet medication. |
Hypertension Hypertension Resistant to Conventional Therapy |
Assistance Publique- Hôpitaux de Paris |
2015-09 | Phase 4 |
Rilmenidine enhances autophagy in wild-type mice. (A) Endogenous LC3-II levels were measured in stable inducible PC12 cells 48 h after switching on expression of either huntingtin exon 1 with 23 polyglutamine repeats (htt-23Q) or 74 polyglutamine repeats (htt-74Q) in the presence or absence of rilmenidine (for the final 24 h). Actin was used as a loading control. (B) LC3-II levels were measured using fluorescent intensity of the bands by Li-Cor Odyssey. Results are shown as a percentage of control in each individual cell line (n = 5, *P < 0.05 by t-test). The increase in LC3-II levels in rilmenidine treated, htt-74Q is not significantly greater than in htt-23Q treated cells, and possible differences may be due to variations between the clonal cell lines used. (C) LC3-II levels in muscle lysates from rilmenidine-treated and placebo-treated wild-type mice after 24 weeks of treatment. Western blots were also probed for tubulin as a loading control (D) Densitometric analysis of LC3-II-levels relative to tubulin. Control condition is set to 100%. Error bars show SEM (*P = 0.036, t-test, n = 4 for rilmenidine, n = 5 for control). (E) In cultured primary cortical neurons, LC3-II levels were assessed by western blot. Two exposures are shown to allow comparison of weaker bands in non-bafilomycin A1-treated lanes (−Baf A1) and stronger bands in bafilomycin A1-treated lanes without saturation. (F) Densitometric quantification of LC3-II levels relative to actin in triplicate experiments. (*P < 0.05 by t-test). Effect of rilmenidine treatment on phosphorylation of downstream mTOR targets was investigated by western blotting, (G) phosphorylated p70 S6 kinase levels, (H) phosphorylated S6 ribosomal protein and (I) phosphorylated 4EBP1. In these experiments, rapamycin treatment was used as a control for the inactivation of mTOR where the effects of treatment can be clearly seen. Hum Mol Genet . 2010 Jun 1;19(11):2144-53. td> |
Rilmenidine treatment improved overall performance at the wire manoeuvre task as well as the severity of tremors at certain time points in N171-82Q mice. (A) Mice were scored on their ability to perform the wire manoeuvre, score: 0, active grip with hind legs; 1, difficulty grasping with hind legs; 2, unable to lift hind legs; 3, falls within 30 s; 4, falls immediately. The percentage of animals obtaining each score is shown in the graphs, black bars represent rilmenidine-treated animals and white bars represent control, placebo-treated animals. Significant differences between treatment groups were seen at 12 weeks (P = 0.002), 14 weeks (P = 0.017), 16 weeks (P = 0.0246), 18 weeks (P = 0.0211) and 20 weeks (P=0.0056) of age (Mann–Whitney U test). No significant differences were seen pre-treatment at 4 weeks as well as at 22 weeks (P = 0.1495) of age. (B) The severity of tremors in N171-82Q mice was significantly improved by rilmenidine treatment at 16 weeks (P = 0.0403) and 18 weeks (P = 0.0293) of age, and a trend towards an improvement was also evident at the age of 12 weeks (P = 0.0583) in comparison to the control group. No significant differences were seen at 14 weeks (P = 0.1762), 20 weeks (P = 0.2987) and 22 weeks (P = 0.3367) of age. Score: 0, no tremor; 1, mild tremor; 2, severe tremor.Hum Mol Genet . 2010 Jun 1;19(11):2144-53. td> |