Rilmenidine Phosphateantihypertensive drug targets the imidazoline receptor CAS# 85409-38-7 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 85409-38-7 | SDF | Download SDF |
| PubChem ID | 198614 | Appearance | Powder |
| Formula | C10H19N2O5P | M.Wt | 278.24 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | >5.68mg/mL in DMSO | ||
| Chemical Name | N-(dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amine;phosphoric acid | ||
| SMILES | C1CC1C(C2CC2)NC3=NCCO3.OP(=O)(O)O | ||
| Standard InChIKey | ZJCOWRFWZOAVFY-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C10H16N2O.H3O4P/c1-2-7(1)9(8-3-4-8)12-10-11-5-6-13-10;1-5(2,3)4/h7-9H,1-6H2,(H,11,12);(H3,1,2,3,4) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
Rilmenidine Phosphate Dilution Calculator
Rilmenidine Phosphate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.594 mL | 17.9701 mL | 35.9402 mL | 71.8804 mL | 89.8505 mL |
| 5 mM | 0.7188 mL | 3.594 mL | 7.188 mL | 14.3761 mL | 17.9701 mL |
| 10 mM | 0.3594 mL | 1.797 mL | 3.594 mL | 7.188 mL | 8.985 mL |
| 50 mM | 0.0719 mL | 0.3594 mL | 0.7188 mL | 1.4376 mL | 1.797 mL |
| 100 mM | 0.0359 mL | 0.1797 mL | 0.3594 mL | 0.7188 mL | 0.8985 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Rilmenidine phosphate is the water soluble form of Rilmenidine. It is an antihypertensive drug targets the imidazoline receptor. [1]
Imidazoline receptor is a family of non-adrenergic high affinity binding site for clonidine, idazoxan, and other imidazoline drugs. [2] There are three types of imidazoline receptor. I-1 mediates sympatho-inhibitory actions to the lower blood pressure; I-2 is allosteric binding site of monamine oxidase and I-3 controls insulin secretion of pancreatic cells. [3]
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. [4] Stimulation of imidazoline I-1 receptor by Rilmenidine activated P38 to induce the expression of FXR. [4]
Mice fed with HFD (high fat diet) had improved hepatic steatosis following the administration of Rilmenidien through the activation of imidazoline I-1 receptor. [4] Imidazoline receptors are involved in the bulbospinal regulation of blood pressure and affect peripheral stimulation. [1] In hypertensive patients, Rilmenidine decreased blood pressure in a dose-dependent mater. In contrast with placebo, Rilmenidine had significantly lowered blood pressures. In addition, Rilmenidine had significantly less incidences of adverse effects than using other drugs for hypertension. [1]
References:
[1] Laurent S, Safar M. Rilmenidine: a novel approach to first-line treatment of hypertension. Am J Hypertens. 1992 Apr;5(4 Pt 2):99S-105S.
[2] Regunathan S, Reis DJ. Imidazoline receptors and their endogenous ligands.Annu Rev Pharmacol Toxicol. 1996;36:511-44.
[3] Head GA, Mayorov DN. Imidazoline receptors, novel agents and therapeutic potential. Cardiovasc Hematol Agents Med Chem. 2006 Jan;4(1):17-32.
[4] Yang PS, Wu HT, Chung HH, Chen CT, Chi CW, Yeh CH, Cheng JT. Rilmenidine improves hepatic steatosis through p38-dependent pathway to higher the expression of farnesoid X receptor. Naunyn Schmiedebergs Arch Pharmacol. 2012 Jan;385(1):51-6.
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