GR 79236 |
| Katalog-Nr.GC12315 |
GR 79236 ist ein hochpotenter, selektiver und oral aktiver Adenosin-A1-Rezeptor-Agonist mit einem Kis von 3,1 nM bzw. 1300 nM für A1- bzw. A2-Rezeptoren.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 124555-18-6
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Chemical Name | (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 | ||
| Formula | C15H21N5O5 | M.Wt | 351.36 |
| Löslichkeit | DMSO: 30 mg/ml,Ethanol: 15 mg/ml,Water: 30 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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