货号:A680393
同义名:
ABT 702 dihydrochloride;ABT-702 dihydrochloride
ABT-702 2HCl是一种强效的非核苷腺苷激酶抑制剂,IC50 为 1.7 nM,在动物疼痛和炎症模型中显示口服活性。
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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]. |
计算器 | ||||
存储液制备 | ![]() |
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 |
CAS号 | 1188890-28-9 |
分子式 | C22H21BrCl2N6O |
分子量 | 536.252 |
别名 | ABT 702 dihydrochloride;ABT-702 dihydrochloride |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere,Store in freezer, under -20°C |
溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |