Rilmenidine (hemifumarate)
(Synonyms: Oxaminozoline,S 3341) 目录号 : GC15657
An antihypertensive agent
Cas No.:207572-68-7
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Rilmenidine is an antihypertensive agent that has been shown to lower arterial pressure in various animal models by inhibiting the tonic activity of sympathoexcitatory neurons in the rostral ventrolateral medulla [1].
In vitro: Bilateral microinjection of rilmenidine into the C1 area of the rostral ventrolateral medulla (RVL) elicited dose-dependent falls in arterial pressure and heart rate. In RVL, rilmenidine competed with binding to imidazole and α2-adrenergic binding sites with a 30-fold selectivity for the imidazole binding sites [2]. Rilmenidine, a new antihypertensive agent, appeared 2.5 and 3.5 times more selective than clonidine and guanfacine, respectively, for medullary IPR sites than for cortical α-adrenoceptors [3]. Rilmenidine targeted the nonadrenergic imidazoline-binding site I1 receptor with the Ki value of 7.1 nM and demonstrated weaker affinity for the I2 receptor with the Ki value of 5.2 μM [4].
In vivo: In rat model of hypertension associated with insulin resistance, rilmenidine ameliorated the deleterious effects of a high-fructose diet, such as weight gain, hypertension, and resistance to the effects of insulin [5]. In a mouse model of Huntington's disease, rilmenidine induced autophagy, attenuated toxicity of polyglutamine expansions and the signs of disease, reduced the mutant huntingtin fragment levels [6].
References:
[1] Reis, D. J. and Piletz, J.E. The imidazoline receptor in control of blood pressure by clonidine and allied drugs. American Journal of Physiology 273(5 Pt 2), R1569-R1571 (1997).
[2] Gomez R E, Ernsberger P, Feinland G, et al. Rilmenidine lowers arterial pressure via imidazole receptors in brainstem C1 area[J]. European journal of pharmacology, 1991, 195(2): 181-191.
[3] Bricca G, Dontenwill M, Molines A, et al. Rilmenidine selectivity for imidazoline receptors in human brain[J]. European journal of pharmacology, 1989, 163(2): 373-377.
[4] Guyenet P G. Is the hypotensive effect of clonidine and related drugs due to imidazoline binding sites [J]. American Journal of Physiology-Regulatory, Integrative and Comparative Physiology, 1997, 273(5): R1580-R1584.
[5] Penicaud L, Berthault M F, Morin J, et al. Rilmenidine normalizes fructose-induced insulin resistance and hypertension in rats[J]. Journal of hypertension. Supplement: official journal of the International Society of Hypertension, 1998, 16(3): S45-9.
[6] Rose C, Menzies F M, Renna M, et al. Rilmenidine attenuates toxicity of polyglutamine expansions in a mouse model of Huntington's disease[J]. Human molecular genetics, 2010, 19(11): 2144-2153.
| Cas No. | 207572-68-7 | SDF | |
| 别名 | Oxaminozoline,S 3341 | ||
| 化学名 | N-(dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine, 2E-butenedioate | ||
| Canonical SMILES | OC(/C=C/C(O)=O)=O.C1(NC(C2CC2)C3CC3)=NCCO1.C4(NC(C5CC5)C6CC6)=NCCO4 | ||
| 分子式 | C10H16N2O • 1/2C4H4O4 | 分子量 | 238.3 |
| 溶解度 | ≤10mg/ml in ethanol;3mg/ml in DMSO;3mg/ml in dimethyl formamide | 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。 |
||
| 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 | 4.1964 mL | 20.982 mL | 41.9639 mL |
| 5 mM | 0.8393 mL | 4.1964 mL | 8.3928 mL |
| 10 mM | 0.4196 mL | 2.0982 mL | 4.1964 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。