S82562 |
GR79236 |
源葉(MedMol) | 98% |
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- 產(chǎn)品描述: GR79236 is a highly potent, selective and orally active adenosine A1 receptor agonist with a Kis of 3.1 nM and 1300 nM for A1 and A2 receptors, respectively. GR79236 has anti-nociceptive and anti-inflammatory actions
- 靶點(diǎn): Ki: 3.1 nM (Adenosine A1 receptor) and 1300 nM (Adenosine A2 receptor);AdenosineReceptor
- 體外研究:
GR79236 inhibits Isoprenaline-stimulated cAMP accumulation in DDT-MF2 cells with an IC50 of 2.6 nM. GR79236 inhibits catecholamine-induced lipolysis in human, rat and dog isolated adipocytes
- 體內(nèi)研究:
GR79236 decreases locomotor activity and inhibits DMCM-induced seizures in mice (ED50s of 0.13 mg/kg and 0.3 mg/kg, respectively). Oral administration of GR79236 (0.1-10 mg/kg) to fed rats induces minimal changes in the plasma concentration of non-esterified fatty acids and in the blood concentrations of glucose and lactate. Intravenous infusion of GR79236 to fasted pithed rats, or oral administration of GR79236 to fasted conscious rats and dogs, produces time- and dose-dependent decreases in the plasma non-esterified fatty acid concentration. In the fasted rats, doses of GR79236 that lowered plasma levels of non-esterified fatty acids also produced hypotriglyceridaemia and anti-ketotic effects
- 參考文獻(xiàn):
1. L J Knutsen, et al. N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects. J Med Chem. 1999 Sep 9;42(18):3463-77. 2. Sneyd JR, et al. Multicentre evaluation of the adenosine agonist GR79236X in patients with dental pain after third molar extraction. Br J Anaesth. 2007 May;98(5):672-676. 3. P Strong, et al. Suppression of non-esterified fatty acids and triacylglycerol in experimental animals by the adenosine analogue GR79236. Clin Sci (Lond). 1993 Jun;84(6):663-9.
- 溶解性: Soluble in DMSO、H2O
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 2.846 ml 14.231 ml 28.461 ml 5 mM 0.569 ml 2.846 ml 5.692 ml 10 mM 0.285 ml 1.423 ml 2.846 ml 50 mM 0.057 ml 0.285 ml 0.569 ml
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輸入產(chǎn)品批號(hào):
本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)