| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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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].
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| ln Vivo |
N171-82Q mice treated with rilmenidine (ip; 4 times per week) demonstrated significant gains in forelimb grip strength and all limb grip strength between 12 and 22 weeks of age [3]. Rilmenidine decreases levels of mutant huntingtin protein [3].
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| 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 |
| Molecular Formula |
C24H36N4O6
|
|---|---|
| Molecular Weight |
476.565846443176
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| Exact Mass |
476.263
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| CAS # |
207572-68-7
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| Related CAS # |
Rilmenidine;54187-04-1
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| PubChem CID |
45073450
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
34
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| Complexity |
338
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC1C(C2CC2)NC3=NCCO3.C1CC1C(C2CC2)NC3=NCCO3.C(=C/C(=O)O)\C(=O)O
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| InChi Key |
LZFATBMLSYHRTC-WXXKFALUSA-N
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| InChi Code |
InChI=1S/2C10H16N2O.C4H4O4/c2*1-2-7(1)9(8-3-4-8)12-10-11-5-6-13-10;5-3(6)1-2-4(7)8/h2*7-9H,1-6H2,(H,11,12);1-2H,(H,5,6)(H,7,8)/b;;2-1+
|
| Chemical Name |
(E)-but-2-enedioic acid;N-(dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amine
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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 (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
H2O : ~50 mg/mL (~209.84 mM)
DMSO : ~10 mg/mL (~41.97 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (4.20 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1 mg/mL (4.20 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (4.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0983 mL | 10.4916 mL | 20.9833 mL | |
| 5 mM | 0.4197 mL | 2.0983 mL | 4.1967 mL | |
| 10 mM | 0.2098 mL | 1.0492 mL | 2.0983 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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