2. Metabolic Enzyme/Protease Neuronal Signaling GPCR/G Protein
  3. Adenosine Kinase Adenosine Receptor
  4. ABT-702

ABT-702 (Adenosine Kinase Inhibitor) 是一种强效、具有口服活性且选择性的腺苷激酶 (AK) 抑制剂，其 IC50 值为 1.7 nM。ABT-702 对腺苷激酶的选择性比对其他生物靶点 (包括环氧合酶 -1和 -2) 的选择性高出 1300 倍以上。ABT-702 通过提高游离腺苷水平来减轻糖尿病视网膜病变中的炎症。ABT-702 在体内表现出镇痛和抗炎作用。ABT-702 可用于糖尿病视网膜病变的相关研究。

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ABT-702

ABT-702 Chemical Structure

CAS No. : 214697-26-4

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5 mg ￥1892
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10 mg ￥3047
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25 mg ￥5192
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Customer Review

Other Forms of ABT-702:

ABT-702 相关抗体

Top Publications Citing Use of Products

查看 Adenosine Receptor 亚型特异性产品:

查看所有亚型
Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ABT-702 (Adenosine Kinase Inhibitor) is a potent, orally active, and selective adenosine kinase (AK) inhibitor with an IC50 of 1.7 nM. ABT-702 shows >1300-fold selectivity for AK over other biological targets, including cyclooxygenases-1 and -2. ABT-702 attenuates inflammation in diabetic retinopathy by increasing free adenosine levels. ABT-702 shows analgesic and anti-inflammatory effects in vivo. ABT-702 can be used for diabetic retinopathy research[1][2][3].

IC50 & Target

IC50: 1.7 nM (Adenosine kinase, AK)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
IMR-32 IC50
50 nM
Compound: 21 (ABT-702)
Inhibition of adenosine phosphorylation in confluent IMR-32 (human neuroblastoma) cells.
Inhibition of adenosine phosphorylation in confluent IMR-32 (human neuroblastoma) cells.
[PMID: 11405650]
体外研究
(In Vitro)

ABT-702 (5-50 μM，30 分钟) 通过 A2AAR 以剂量依赖的方式抑制 amadori 糖化白蛋白 (AGA) 诱导的小胶质细胞中 TNF-α 的释放[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ABT-702 相关抗体:
体内研究
(In Vivo)

ABT-702 (0.6-100 µmol/kg，腹腔注射或口服，单次给药) 在大鼠中显示出剂量依赖性的镇痛和抗炎作用[1]。
ABT-702 (1.5 mg/kg，腹腔注射，每周两次，持续 8 周) 通过减轻视网膜炎症、氧化应激和细胞死亡来改善小鼠的糖尿病视网膜病变[2]。
ABT-702 (3 mg/kg，腹腔注射，于 FDG 注射前 10 分钟给药) 可在大鼠小脑、中脑区及延髓诱导显著的局部代谢减退[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male rats[1]
Dosage: 0.6-100 µmol/kg
Administration: i.p., single dose
Result: Showed potent, dose-dependent antinociceptive effects across multiple pain models, including inflammatory thermal hyperalgesia, formalin test, and nerve injury-induced tactile allodynia.
Demonstrated significant anti-inflammatory effects by reducing carrageenan-induced paw edema.
Exhibited a non-opioid mechanism of action, as its effects were not reversed by the opioid antagonist naloxone.
Showed less potential for developing antinociceptive tolerance compared to morphine.
Animal Model: Male rats[1]
Dosage: 5-100 µmol/kg
Administration: p.o., single dose
Result: Showed potent, dose-dependent antinociceptive effects across multiple pain models, including inflammatory thermal hyperalgesia, formalin test, and nerve injury-induced tactile allodynia.
Demonstrated significant anti-inflammatory effects by reducing carrageenan-induced paw edema.
The antinociceptive and anti-inflammatory effects were blocked by selective adenosine receptor antagonists, confirming an adenosine-dependent mechanism.
Exhibited a non-opioid mechanism of action.
Showed less potential for developing antinociceptive tolerance compared to morphine.
Had no significant effects on exploratory locomotor activity at lower analgesic doses.
Reduced locomotor activity but did not impair motor coordination at higher doses.
Had no significant effects on heart rate or mean arterial pressure at doses providing maximal anti-hyperalgesia.
Animal Model: Male C57BL/6J (8 weeks) intraperitoneally injected with Streptozotocin (45 mg/kg, 5 consecutive days) to induce diabetes[2]
Dosage: 1.5 mg/kg
Administration: i.p., twice a week for 8 weeks
Result: Showed no effects on final body weight and blood glucose levels in diabetic mice.
Showed lower signs of inflammation (ICAM-1, TNF-α, and microglial activation marker Iba1) compared to control animals receiving the vehicle.
Suppressed the upregulation of A₂A receptor and reduced ENT1 expression.
Reduced oxidative and nitrosative stress in the retina.
Blocked the diabetic effect on AK in diabetic mice as compared with vehicle-treated diabetic mice.
Blocked cell death (decreased cleaved caspase-3 and TUNEL-positive cells) in diabetic mice but did not affect treated normal controls.
Animal Model: Rats[3]
Dosage: 3 mg/kg
Administration: i.p., 10 minutes pre-FDG
Result: Showed significant regional hypometabolism in the cerebellum, mesencephalic region, and medulla compared to the vehicle-treated rats.
分子量

463.33

Formula

C22H19BrN6O
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 25 mg/mL (53.96 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1583 mL 10.7914 mL 21.5829 mL
5 mM 0.4317 mL 2.1583 mL 4.3166 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

ABT-702 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1583 mL 10.7914 mL 21.5829 mL 53.9572 mL
5 mM 0.4317 mL 2.1583 mL 4.3166 mL 10.7914 mL
10 mM 0.2158 mL 1.0791 mL 2.1583 mL 5.3957 mL
15 mM 0.1439 mL 0.7194 mL 1.4389 mL 3.5971 mL
20 mM 0.1079 mL 0.5396 mL 1.0791 mL 2.6979 mL
25 mM 0.0863 mL 0.4317 mL 0.8633 mL 2.1583 mL
30 mM 0.0719 mL 0.3597 mL 0.7194 mL 1.7986 mL
40 mM 0.0540 mL 0.2698 mL 0.5396 mL 1.3489 mL
50 mM 0.0432 mL 0.2158 mL 0.4317 mL 1.0791 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ABT-702214697-26-4ABT702ABT 702Adenosine KinaseAdenosine ReceptorADKP1 receptoradenosine kinasediabetic retinopathyanalgesicA2AARInhibitorinhibitorinhibit

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