|5-(3-溴苯基)-7-(6-吗啉吡啶-3-基)吡啶并[2,3-d]嘧啶-4-胺二盐酸盐|CsnPharm

CAS No.: 1188890-28-9

ABT-702 2HCl/ABT 702二盐酸盐 Catalog No. CSN21069

Synonyms: ABT 702 2HCl;ABT 702 Dihydrochloride;ABT-702

ABT702 2HCl is a potent non-nucleoside adenosine kinase inhibitor with IC50 value of 1.7 nM, displaying oral activity in animal models of pain and inflammation.

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400-920-2911

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技术信息

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 (AK_long and AK_short), 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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8648 mL
- 9.3240 mL
- 18.6480 mL
- 5 mM
- 0.3730 mL
- 1.8648 mL
- 3.7296 mL
- 10 mM
- 0.1865 mL
- 0.9324 mL
- 1.8648 mL

技术信息

CAS号

1188890-28-9

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H21BrCl2N6O

运输

蓝冰

分子量

536.25

别名

ABT 702 2HCl;ABT 702 Dihydrochloride;ABT-702;ABT-702 HCl;ABT-702 hydrochloride

溶解度

DMSO	225.0 mg/mL (419.6 mM)
Water	insoluble

动物实验配方

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ABT-702 2HCl/ABT 702二盐酸盐 Catalog No. CSN21069

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