Sumanirole (Synonyms: PNU-95666E)

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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.

For research use only. We do not sell to patients.

Sumanirole Chemical Structure

CAS No. : 179386-43-7

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Other In-stock Forms of Sumanirole:

Sumanirole maleate

Other Forms of Sumanirole:

Sumanirole maleate In-stock

1 Publications Citing Use of MCE Sumanirole

•Biomed Pharmacother. 2021, 111500.

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

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]

Molecular Weight

203.24

Formula

C₁₁H₁₃N₃O

CAS No.

179386-43-7

SMILES

O=C1NC2=CC=CC3=C2N1C[C@H](NC)C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Arthur G. Romero, et al. Synthesis of the Selective D2 Receptor Agonist PNU-95666E from D-Phenylalanine Using a Sequential Oxidative Cyclization Strategy. J. Org. Chem. 1997, 62, 6582-6587

Sumanirole Related Classifications

Neurological Disease

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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