Rilmenidine Phosphate
(Synonyms: 磷酸利美尼定) 目录号 : GC13017
An antihypertensive agent
Cas No.:85409-38-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| Cas No. | 85409-38-7 | SDF | |
| 别名 | 磷酸利美尼定 | ||
| 化学名 | N-(dicyclopropylmethyl)-4,5-dihydrooxazol-2-amine phosphate | ||
| Canonical SMILES | OP(O)(O)=O.C1(NC(C2CC2)C3CC3)=NCCO1 | ||
| 分子式 | C10H19N2O5P | 分子量 | 278.24 |
| 溶解度 | ≥ 5.68mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.594 mL | 17.9701 mL | 35.9402 mL |
| 5 mM | 0.7188 mL | 3.594 mL | 7.188 mL |
| 10 mM | 0.3594 mL | 1.797 mL | 3.594 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。