GR 79236
目录号 : GC12315
An adenosine A1 receptor agonist
Cas No.:124555-18-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 3.1 nM (Ki)
GR 79236, N-[(1 S, trans)-2-hydroxycyclopentyl] adenosine, is an highly potent and selective adenosine A1 receptor agonist. Adenosine A1 receptor is ubiquitous throughout the entire body, and ofter has an inhibitory function on most of the tissues.
In vitro: GR79236 is a highly potent and selective A1 receptor agonist which is originally developed for the treatment of Type 2 diabetes mellitus, as a cardioprotective agent and also for peripheral arterial occlusive diseases. GR79236 inhibited catecholamine-induced lipolysis in adipocytes at low concentrations [1]
In vivo: GR79236 has a pronounced effect on NEFA and TG levels in both acute and chronic animal models, thus establishing the potential of this approach for the treatment of T2D [1]. GR79236 also can inhibit neurogenic vasodilation in anaesthetized rats, inhibit electrical stimulation of superior saggital sinusinduced trigeminovascular nociceptive transmission and CGRP release in anaesthetized cats and inhibit trigeminal nociception in humans [2].
Clinical trial: The analgesic efficacy of GR79236 was evaluated in the dental pain model (primarily inflammatory pain state). No evidence of efficacy of GR79236 was found compared with placebo [3].
References:
[1] Kiesman WF, Elzein E, Zablocki J. A1 adenosine receptor antagonists, agonists, and allosteric enhancers. Handb Exp Pharmacol. 2009;(193):25-58.
[2] Arulmani U, Heiligers JP, Centurión D, Garrelds IM, Villalón CM, Saxena PR. Lack of effect of the adenosine A1 receptor agonist, GR79236, on capsaicin-induced CGRP release in anaesthetized pigs. Cephalalgia. 2005 Nov;25(11):1082-90.
[3] Sneyd JR, Langton JA, Allan LG, Peacock JE, Rowbotham DJ. Multicentre evaluation of the adenosine agonist GR79236X in patients with dental pain after third molar extraction. Br J Anaesth. 2007 May;98(5):672-6. Epub 2007 Apr 7.
| Cas No. | 124555-18-6 | SDF | |
| 化学名 | (2S,3R,4S,5R)-2-(6-(((1S,2S)-2-hydroxycyclopentyl)amino)-9H-purin-9-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol | ||
| Canonical SMILES | O[C@H]1[C@@H](N2C3=NC=NC(N[C@@H](CCC4)[C@H]4O)=C3N=C2)O[C@H](CO)[C@H]1O | ||
| 分子式 | C15H21N5O5 | 分子量 | 351.36 |
| 溶解度 | DMSO: 30 mg/ml,Ethanol: 15 mg/ml,Water: 30 mg/ml | 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 | 2.8461 mL | 14.2304 mL | 28.4608 mL |
| 5 mM | 0.5692 mL | 2.8461 mL | 5.6922 mL |
| 10 mM | 0.2846 mL | 1.423 mL | 2.8461 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。