Moxonidine
(Synonyms: 莫索尼定; BDF5895) 目录号 : GC12629
An imidazoline I1 and α2A-adrenergic receptor agonist
Cas No.:75438-57-2
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
Moxonidine is an agonist of I1-imidazoline receptor with EC50 value of 1.3µM [1].
Moxonidine can bind to both I1-imidazoline receptor (I1R) and α2-adrenergic receptor (α2AR). The selectivity of moxonidine for I1R is 33-fold over α2AR. Moxonidine plays its antihypertensive role in the central nervous system. It has a central site of action. It is shown no effect in pithed rats and in cats following spinal cord transaction. Moxonidine also reduces sympathetic outflow and lowers peripheral vascular resistence [1, 2].
Besides the antihypertensive efficacy, Moxonidine is reported to have effects on gastric secretion and gastric mucosal injury in rats. It significantly reduces basal gastric acid secretion when given doses of 0.1 (63% inhibition) and 1.0 (65% inhibition) mg/kg. Even 0.01mg/kg moxonidine can reduce the gastric mucosal injury induced by ethanol [3].
References:
[1] George OK, Gonzalez RR Jr, Edwards LP. Moxonidine, an antihypertensive agent, is permissive to alpha1-adrenergic receptor pathway in the rat-tail artery. J Cardiovasc Pharmacol. 2004 Feb;43(2):306-11.
[2] Morris ST, Reid JL. Moxonidine: a review. J Hum Hypertens. 1997 Oct;11(10):629-35.
[3] Glavin GB, Smyth DD. Effects of the selective I1 imidazoline receptor agonist, moxonidine, on gastric secretion and gastric mucosal injury in rats. Br J Pharmacol. 1995 Feb;114(4):751-4.
| Cas No. | 75438-57-2 | SDF | |
| 别名 | 莫索尼定; BDF5895 | ||
| 化学名 | 4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methylpyrimidin-5-amine | ||
| Canonical SMILES | CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC | ||
| 分子式 | C9H12ClN5O | 分子量 | 241.68 |
| 溶解度 | ≥ 11.3 mg/mL in DMSO, ≥ 4.74 mg/mL in EtOH with ultrasonic | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.1377 mL | 20.6885 mL | 41.377 mL |
| 5 mM | 0.8275 mL | 4.1377 mL | 8.2754 mL |
| 10 mM | 0.4138 mL | 2.0689 mL | 4.1377 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。