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ABT 702 dihydrochloride

现货
Catalog No.
B5298
腺苷激酶抑制剂
组合的产品项目
规格价格库存 数量
10mg
¥ 3,980.00
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Background

IC50: 1.7 nM for adenosine kinase

Adenosine (ADO) is an endogenous homeostatic inhibitory neuromodulator that reduces cellular excitability at sites of tissue injury and inflammation. Inhibition of adenosine kinase (AK), the primary metabolic enzyme for ADO, selectively increases ADO concentrations at sites of tissue trauma and enhances the analgesic and antiinflammatory actions of ADO. ABT 702 is a novel, potent nonnucleoside AK inhibitor.

In vitro: ABT 702 was active both in inhibiting AK (IC50 ) 1.7 nM) and ADO phosphorylation in the intact cells (IC50 ) 50 nM). ABT 702 was also highly selective for AK inhibition as compared to other sites of ADO action including ADA, ADO receptors, and ADO transport sites [1].

In vivo: ABT 702 had dose-dependent antinociceptive and antiinflammatory actions in a variety of animal models of nociceptive, inflammatory, and neuropathic pain. ABT 702 is the first of a novel class of potent, selective, non-nucleoside, orally active AK inhibitors that have potent antinociceptive effects in animal models [1].

Clinical trial: Up to now, ABT 702 is still in the preclinical development stage.

Reference:
[1] Lee CH, Jiang M, Cowart M, Gfesser G, Perner R, Kim KH, Gu YG, Williams M, Jarvis MF, Kowaluk EA, Stewart AO, Bhagwat SS.  Discovery of 4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin-3-yl)pyrido[2,3-d]pyrimidine, an orally active, non-nucleoside adenosine kinase inhibitor.. J Med Chem. 2001 Jun 21;44(13):2133-8.

Chemical Properties

Physical AppearanceOrange solid
StorageStore at -20°C
M.Wt536.26
Cas No.1188890-28-9
FormulaC22H19N6OBr.2HCl
Solubility≥107.2 mg/mL in DMSO, ≥9.84 mg/mL in EtOH with ultrasonic and warming, <2.69 mg/mL in H2O
Chemical Name5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2,3-d]pyrimidin-4-amine dihydrochloride
SDFDownload SDF
Canonical SMILESBrC1=CC=CC(C2=CC(C3=CN=C(N4CCOCC4)C=C3)=NC5=NC=NC(N)=C25)=C1.Cl.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

化学结构

ABT 702 dihydrochloride