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Adenosine Kinase Inhibitor(hydrate)
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。
Adenosine Kinase Inhibitor(hydrate)图片
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
inhibitor of adenosine kinase
别名ABT-702
化学名5-(3-bromophenyl)-7-[6-(4-morpholinyl)-3-pyridinyl]-pyrido[2,3-d]pyrimidin-4-amine, hydrate (5:2)
Canonical SMILESBrC1=CC=CC(C2=CC(C3=CN=C(N4CCOCC4)C=C3)=NC5=C2C(N)=NC=N5)=C1.O
分子式C22H19BrN6O o 0.4H2O
分子量470.5
溶解度≤30mg/ml in DMSO;20mg/ml in dimethyl formamide
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: 1.7 nM in cell-free assays

Adenosine Kinase Inhibitor is an inhibitor of adenosine kinase.

Adenosine kinase is the key metabolizing enzyme regulating cellular adenosine concentrations. Inhibition of adenosine kinase can selectively enhance the protective actions of adenosine during tissue trauma without producing the nonspecific effects associated with the systemic administration of adenosine receptor agonists.

In vitro: Adenosine Kinase Inhibitor was found to be a potent non-nucleoside adenosine kinase inhibitor with several folds of magnitude selectivity over other sites of adenosine interaction. Adenosine Kinase Inhibitor was 1300- to 7700-fold selective for adenosine kinase compared with other neurotransmitter and peptide receptors, neurotransmitter/nucleoside reuptake sites, and enzymes. Adenosine Kinase Inhibitor was equipotent in inhibiting native human adenosine kinase, human recombinant isoforms, as well as adenosine kinase from dog, rat, monkey, and mouse brain [1].

In vivo: Adenosine Kinase Inhibitor was orally active and efficacious in reducing acute somatic nociception in the mouse hot-plate assay. Adenosine Kinase Inhibitor could dose-dependently reduce nociception in the phenyl-p-quinone-induced abdominal constriction assay. The antinociceptive effects of Adenosine Kinase Inhibitor in the hotplate assay were stop by the nonselective adenosine receptor antagonist theophylline, but not by a peripherally selective adenosine receptor antagonist [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Jarvis, M. F.,Yu, H.,Kohlhaas, K., et al. ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin-3-yl)pyrido[2,3-d]pyrimidine, a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse. Journal of Pharmacology and Experimental Therapeutics 295(3), 1156-1164 (2000).