2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. Sumanirole

Sumanirole (PNU-95666E) 是高度选择性的 D2 受体完全激动剂，ED50 为 46 nM。Sumanirole 在帕金森病和不宁腿综合征的研究中发挥着重要作用。

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Sumanirole Chemical Structure

Sumanirole Chemical Structure

CAS No. : 179386-43-7

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Sumanirole 的其他形式现货产品:

Other Forms of Sumanirole:

Sumanirole 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

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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

Sumanirole (PNU-95666E) is a highly selective D2 receptor full agonist with an ED50 of about 46 nM. Sumanirole plays an important role in the research of Parkinson's disease and restless leg syndrome[1].

IC50 & Target

D2 Receptor

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
4.6 nM
Compound: 1; Sumanirole; U-95666E; PNU-95666E
Agonist activity at recombinant human D2 receptor expressing in CHO cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation by beta plate counter
Agonist activity at recombinant human D2 receptor expressing in CHO cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation by beta plate counter
[PMID: 27035329]
HEK293 EC50
10.8 nM
Compound: 3 (PNU-95666E)
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay
[PMID: 15239663]
HEK293 EC50
165 nM
Compound: 3 (PNU-95666E)
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D2 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D2 using FLIPR assay
[PMID: 15239663]
HEK293 EC50
32.2 nM
Compound: 1
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay
[PMID: 28300398]
HEK293 EC50
35 nM
Compound: 3 (PNU-95666E)
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assay
[PMID: 15239663]
HEK293 EC50
501.2 nM
Compound: 1
Agonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assay
Agonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assay
[PMID: 28300398]
HEK293 EC50
543.3 nM
Compound: 1
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assay
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assay
[PMID: 28300398]
HEK293 EC50
74.8 nM
Compound: 1
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assay
Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assay
[PMID: 28300398]
HEK-293T EC50
186 nM
Compound: 1; Sumanirole; U-95666E; PNU-95666E
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
[PMID: 27035329]
HEK-293T EC50
60.1 nM
Compound: 1; Sumanirole; U-95666E; PNU-95666E
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay
[PMID: 27035329]
Clinical Trial
分子量

203.24

Formula

C11H13N3O
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

Sumanirole 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:

Sumanirole179386-43-7PNU-95666EDopamine ReceptorD2receptorParkinson'sdiseaserestlesslegsyndromeInhibitorinhibitorinhibit

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目录号：
HY-70081
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