Sumanirole
(Synonyms: PNU-95666E)
3 Cited Publications
Revisión del cliente
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.
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- No. CAS: 179386-43-7
- Fòrmula: C11H13N3O
- Peso molecular:203.24
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) Sumanirole
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Actividad biológica
Descripciòn
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
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D2 Receptor |
Cellular Effect
|
Cell Line
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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
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[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] |
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 179386-43-7
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Peso molecular 203.24
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Fòrmula C11H13N3O
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SMILES
O=C1NC2=CC=CC3=C2N1C[C@H](NC)C3
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Synonyms
PNU-95666E
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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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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
Pureza y Documentación
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Pureza:
99.98%
Assay:
99.98%
ee.:
99.98%
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Sumanirole Related Classifications
HY-70081 Related Classifications
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