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ABT-702 dihydrochloride

产品编号 T4668 CAS 1188890-28-9

ABT-702 dihydrochloride 是腺苷激酶抑制剂，IC50为1.7 nM。

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ABT-702 dihydrochloride Chemical Structure

ABT-702 dihydrochloride, CAS 1188890-28-9

规格	价格/CNY	货期
1 mg	￥ 473	现货
2 mg	￥ 738	现货
5 mg	￥ 1,280	现货
10 mg	￥ 1,980	现货
25 mg	￥ 3,490	现货
50 mg	￥ 4,970	现货
100 mg	￥ 7,220	现货
500 mg	￥ 14,300	现货
1 mL * 10 mM (in DMSO)	￥ 1,670	现货

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其他形式的 ABT-702 dihydrochloride:

ABT 702 hydrochloride
询价

选择批次

纯度: 98.89%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	ABT-702 dihydrochloride is a potent adenosine kinase (AK) inhibitor.
靶点活性	Adenosine kinase:1.7nM
体外活性	ABT-702 is an orally effective adenosine kinase inhibitor that has several orders of magnitude selectivity over other sites of adenosine (ADO) interaction (A1, A2A, A3 receptors, ADO transporter, and ADO deaminase). ABT-702 is 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.ABT-702 also potently inhibits AK activity in intact cultured IMR-32 human neuroblastoma cells (IC50=51 nM), indicating that ABT-702 can penetrate the cell membrane and potently inhibit AK at its intracellular site.
体内活性	Rats are given an intraperitoneal injection of the adenosine A1 receptor antagonist DPCPX (3 mg/kg), ABT-702 (3 mg/kg), or vehicle 10 minutes prior to an intravenous injection of 2-18F-fluorodeoxy-D-glucose (FDG) (FDG, 15.4±0.7 MBq per rat). Rats are then subjected to a 15 minute static positron emission tomography (PET) scan. Reconstructed images are normalized to FDG PET template for rats and standard uptake values (SUVs) are calculated. To examine the regional effect of active treatment compared to vehicle, statistical parametric mapping analysis is performed. Whole-brain FDG uptake is not affected by drug treatment. Significant regional hypometabolism is detected, particularly in cerebellum, of DPCPX and ABT-702 treated rats, relative to vehicle-treated rats. Thus, endogenous adenosine can affect FDG accumulation although this effect is modest in quiescent rats. Body weight (316.8±28.4 g; mean±SD) and blood glucose (5.5±1.7 mM) are not significantly different among three groups. Whole-brain PET SUV values are 1.6±0.4, 1.6±0.6, and 1.8±0.6 for vehicle, ABT-702, and DPCPX-treated rats, respectively (F(2,9)=0.298, P=0.75). statistical parametric mapping (SPM) analysis reveals significant regional hypometabolism in the cerebellum, mesenceph.ABT-702 significantly reduces acute thermal nociception in a dose-dependent manner after both intraperitoneal (ED50=8 μmol/kg i.p.) and oral (ED50=65 μmol/kg p.o.) administration in the mouse hot-plate test. Consistent with its antinociceptive effects in the hot-plate assay, ABT-702 also produces dose-dependent antinociceptive effects (ED50=2 μmol/kg i.p.) in the abdominal constriction assay.
动物实验	Rats are fasted for 16 hours prior to use. At the beginning of the experiment, each rat is weighed, and then anesthetized using 5% isoflurane for induction and 2.5% for maintenance. A blood sample from tail vein is collected for a fasting blood glucose determination using a standard glucometer. Rats are then given an intraperitoneal (i.p.) injection of DPCPX (3 mg/kg, n=4), ABT-702 (3 mg/kg, n=4), or an equivalent volume of vehicle (15% dimethyl sulfoxide, 15% cremophor EL, 70% saline, n=4) to manipulate the effect of endogenous adenosine on neuronal activities. Ten minutes after i.p. injection, rats are administered FDG (15.4±0.7 MBq) in 0.3-0.5 mL saline by intravenous (i.v.) tail vein injection. Rats are allowed to recover from anesthesia after the FDG injection but are reanesthetized for 15-minute-static PET scan with the head in the center of the field of view.

分子量	536.25
分子式	C22H21BrCl2N6O
CAS No.	1188890-28-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 45 mg/mL (83.91 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8648 mL	9.324 mL	18.648 mL	46.62 mL
	5 mM	0.373 mL	1.8648 mL	3.7296 mL	9.324 mL
	10 mM	0.1865 mL	0.9324 mL	1.8648 mL	4.662 mL
	20 mM	0.0932 mL	0.4662 mL	0.9324 mL	2.331 mL
	50 mM	0.0373 mL	0.1865 mL	0.373 mL	0.9324 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

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质量

配液浓度

参考文献

1. Jarvis MF, 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 2.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, et al. The Effect of Endogenous Adenosine on Neuronal Activity in Rats: An FDG PET Study. J Neuroimaging. 2016 Jul;26(4):403-5.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

ABT-702 dihydrochloride 1188890-28-9 GPCR/G Protein Neuroscience Adenosine Receptor ABT702 dihydrochloride ADK ABT 702 Dihydrochloride Inhibitor inhibit ABT-702 Adenosine Kinase ABT 702 ABT 702 dihydrochloride ABT-702 Dihydrochloride ABT702 ABT702 Dihydrochloride inhibitor

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ABT-702 dihydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

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剂量换算

体内实验配液计算器

技术支持

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