2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. ABT-724

ABT-724 是一种有效且高度选择性的多巴胺 D4 受体激动剂，对人多巴胺 D4 受体的 EC50 为 12.4 nM。ABT-724 是大鼠 D4 (EC50 为 14.3 nM) 和雪貂 D4 受体 (EC50 为 23.2 nM) 的有效部分激动剂，对多巴胺 D1，D2，D3 或 D5 受体没有影响。ABT-724 可用于研究勃起功能障碍，并具有较少的副作用。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 ABT-724 trihydrochloride 通常具有更好的水溶性和稳定性。

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ABT-724 Chemical Structure

ABT-724 Chemical Structure

CAS No. : 70006-24-5

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ABT-724 的其他形式现货产品:

Customer Review

Other Forms of ABT-724:

ABT-724 相关抗体

Top Publications Citing Use of Products

查看 Dopamine Receptor 亚型特异性产品:

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Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ABT-724 is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile[1].

IC50 & Target

EC50: 12.4 nM (Human dopamine D4 receptor), 14.3 nM (Rat dopamine D4 receptor) and 23.2 nM (Ferret dopamine D4 receptor)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
12.4 nM
Compound: 1a, ABT-724
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
[PMID: 17149874]
HEK293 EC50
12.4 nM
Compound: 1 (ABT-724)
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
[PMID: 15239663]
HEK293 EC50
12.4 nM
Compound: 3a
D4 efficacy was measured using recombinant human Dopamine receptor D4 expressed in HEK293 cells
D4 efficacy was measured using recombinant human Dopamine receptor D4 expressed in HEK293 cells
[PMID: 15084133]
HEK293 EC50
13.7 nM
Compound: 1a, ABT-724
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
[PMID: 17149874]
HEK293 EC50
14.3 nM
Compound: 1 (ABT-724)
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
[PMID: 15239663]
HEK293 EC50
23.2 nM
Compound: 1 (ABT-724)
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
[PMID: 15239663]
体外研究
(In Vitro)

ABT-724 exhibits a selective biochemical profile, as indicates by a lack of binding affinity for >70 neurotransmitter/uptake/ion channels including D2, D3, or D5 receptors up to a 10 μM concentration. A weak affinity to 5-HT1A receptors (Ki = 2780 nM) is observed. ABT-724 does not inhibit the PDE activity of PDE1, PDE5, or PDE6 at 10 μM concentrations[1].

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

ABT-724 相关抗体:
体内研究
(In Vivo)

ABT-724 (8.8 μg/kg; subcutaneous injection; daily; for 5 days; male adult Wistar rats) treatment dose-dependently facilitates penile erection when given s.c. to conscious rats[1].

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

Animal Model: Male adult Wistar rats (~300 g)[1]
Dosage: 8.8 μg/kg
Administration: Subcutaneous injection; daily; for 5 days
Result: Dose-dependently facilitated penile erection.
分子量

293.37

Formula

C17H19N5
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ABT-724 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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-72470006-24-5ABT724ABT 724Dopamine ReceptorDopamineD4-receptorpenileerectionpotentiation,side-effectInhibitorinhibitorinhibit

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