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GR 79236
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GR 79236图片
CAS NO:124555-18-6
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
GR 79236 是一种高效、选择性和口服活性的腺苷 A1 受体激动剂,对 A1 和 A2 受体的 Kis 分别为 3.1 nM 和 1300 nM。
Cas No.124555-18-6
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 SMILESO[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℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.