Sumanirole
Based on 3 publication(s) in Google Scholar
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 179386-43-7
- 分子式: C11H13N3O
- 分子量:203.24
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
MedChemExpress(MCE)の使用を引用している文献 Sumanirole
MoreDopamine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
|
D2 Receptor |
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] |
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 179386-43-7
-
分子量 203.24
-
分子式 C11H13N3O
-
SMILES
O=C1NC2=CC=CC3=C2N1C[C@H](NC)C3
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別名
PNU-95666E
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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bioRxiv
2025 Aug 12:2025.08.08.668522. PMID: 40832361 -
Biomed Pharmacother
Dopamine receptor agonists ameliorate bleomycin-induced pulmonary fibrosis by repressing fibroblast differentiation and proliferation. [Abstract]2021 Jul:139:111500. PMID: 33901873
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)