celestialProduct Data Sheet第69届金球奖
Product Name:MDA 19
Cat. No.:GC365792011浙江高考英语
普林斯顿Chemical Properties
国旗下讲话期末考试Cas No.1048973-47-2
Chemical
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N/A2016英语四级
重走青春路
Canonical
SMILES
英语三级听力
O=C(N/N=C1C(N(CCCCCC)C2=C\1C=CC=C2)=O)C3=CC=CC=C3
Formula C21H23N3O2M.Wt349.43 Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , plea warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for veral months.
Shipping Condition Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request.
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Structure
Background
MDA 19 is a lective human CB2 receptor agonist with Ki of 43.3 nM. IC50 Value: 43.3 nM(Ki)Target: CB2 receptorin vitro: MDA19 displayed 4-fold-higher affinity at the human CB(2) than at the human CB1 receptor (K(i) = 43.3 +/-
Product Data Sheet
10.3 vs 162.4 +/- 7.6 nM) and nearly 70-fold-higher affinity at the rat CB2 than at the rat CB1 receptor (K(i) = 16.3 +/- 2.1 vs 1130 +/- 574 nM). In guanosine triphosphate (GTP)gamma[(35)S] functional assays, MDA19 behaved as an agonist at the human CB1 and CB2 receptors and at the r
at CB1 receptor but as an inver agonist at the rat CB2 receptor. In 3’,5’-cyclic adenosine monophosphate (cAMP) assays, MDA19 behaved as an agonist at the rat CB1 receptor and exhibited no functional activity at the rat CB(2) receptor. In extracellular signal-regulated kinas 1 and 2 activation assays, in vivo: MDA19 behaved as an agonist at the rat CB2 receptor. MDA19 attenuated tactile allodynia produced by spinal nerve ligation or paclitaxel in a do-related manner in rats and CB2(+/+) mice but not in CB2(-/-) mice, indicating that CB2 receptors mediated the effects of MDA19. MDA19 did not affect rat locomotor activity.
[1]. Diaz, Philippe; Xu, Jijun; Astruc-Diaz, Fanny et al. Design and Synthesis of a Novel Series of N-Alkyl Isatin Acylhydrazone Derivatives that Act as Selective Cannabinoid Receptor 2 Agonists for the Treatment of Neuropathic Pain. Journal of Medicinal Chemi [2]. Xu JJ, Diaz P, Astruc-Diaz F et al. Pharmacological characterization of a novel cannabinoid ligand, MDA19, for treatment of neuropathic pain. Anesth Analg. 2010 Jul;111(1):99-109.
