| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
Rilmenidine (S-3341), an oxazole analogue, 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 effectiveness of rimedine as an antihypertensive is similar to that of angiotensin-converting enzyme (ACE) inhibitors, beta-blockers, calcium channel blockers, and diuretics [1]. The growth of K562 cells is inhibited by rilmenidine (25–100 μM; 24 hours) [2].
|
|---|---|
| ln Vivo |
Between 12 and 22 weeks of age, N171-82Q mice given rilmenidine (ip; four times per week) shown a significant improvement in all limb grip strength as well as forelimb grip strength [3]. Mutant huntingtin protein levels are lowered by rilmenidine [3].
|
| Cell Assay |
Cell viability assay [2]
Cell Types: K562 Cell Tested Concentrations: 25, 50, 100 μM Incubation Duration: 24 hrs (hours) Experimental Results: Dose-dependent inhibition of K562 colony formation. |
| References | |
| Additional Infomation |
Rilmenidine is an isourea.
Rilmenidine has been used in trials studying the treatment of Hypertension and Chronic Kidney Disease. Oxazole derivative that acts as an agonist for ALPHA-2 ADRENERGIC RECEPTORS and IMIDAZOLINE RECEPTORS. It is used in the treatment of HYPERTENSION. |
| Molecular Formula |
C10H16N2O
|
|---|---|
| Molecular Weight |
180.24684
|
| Exact Mass |
180.126
|
| CAS # |
54187-04-1
|
| Related CAS # |
Rilmenidine hemifumarate;207572-68-7;Rilmenidine phosphate;85409-38-7;Rilmenidine-d4;85047-14-9
|
| PubChem CID |
68712
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
1.2
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
13
|
| Complexity |
219
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
CQXADFVORZEARL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C10H16N2O/c1-2-7(1)9(8-3-4-8)12-10-11-5-6-13-10/h7-9H,1-6H2,(H,11,12)
|
| Chemical Name |
Oxazolidine, 2-((dicyclopropylmethyl)imino)-
|
| Synonyms |
Rilmenidine S 3341 S3341 S-3341
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 5.5479 mL | 27.7393 mL | 55.4785 mL | |
| 5 mM | 1.1096 mL | 5.5479 mL | 11.0957 mL | |
| 10 mM | 0.5548 mL | 2.7739 mL | 5.5479 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.
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