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ABT-702 2HCl

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Chemical Structure| 1188890-28-9 同义名 : ABT 702 dihydrochloride
CAS号 : 1188890-28-9
货号 : A680393
分子式 : C22H21BrCl2N6O
纯度 : 99%+
分子量 : 536.252
MDL号 : MFCD03452809
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(65.27 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Adenosine (ADO) is an inhibitory neuromodulator that can increase nociceptive thresholds in response to noxious stimulation. Inhibitors of the ADO-metabolizing enzyme adenosine kinase (AK) may have therapeutic potential as analgesic and anti-inflammatory agents. ABT702 2HCl is a novel and potent non-nucleoside AK inhibitor with an IC50 value of 0.7 nM. It has oral activity in animal models of inflammation and pain. ABT702 was equipotent (IC50 = 1.5 ± 0.3 nM) in inhibiting native human AK (placenta), two human recombinant isoforms (AKlong and AKshort), and AK from monkey, dog, rat, and mouse brain. ABT702 is orally active and fully efficacious in reducing acute somatic nociception (ED50 = 8 μmol/kg i.p.; 65 μmol/kg p.o.) in the mouse hot-plate assay. ABT702 also dose dependently reduced nociception in the phenyl-p-quinone-induced abdominal constriction assay[1]. Significant regional hypometabolism was detected of ABT702 (3 mg/kg; intraperitoneal injection) treated rats, relative to vehicle-treated rats[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.86mL

0.37mL

0.19mL

9.32mL

1.86mL

0.93mL

18.65mL

3.73mL

1.86mL
参考文献

[1]Jarvis MF, Yu H, et al. ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-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. J Pharmacol Exp Ther. 2000 Dec;295(3):1156-64

[2]Parkinson FE, Paul S, Zhang D, Mzengeza S, Ko JH. The Effect of Endogenous Adenosine on Neuronal Activity in Rats: An FDG PET Study. J Neuroimaging. 2016 Jul;26(4):403-5