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Tocris/Sumanirole maleate/2773/10/10 mg

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货号: 2773/10

品牌: Tocris

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Description: D₂-selective agonist

Chemical Name: (R)-5,6-Dihydro-5-(methylamino)-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (2Z)-2-butenedioate

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

High affinity D₂ receptor agonist (EC₅₀ values are between 17 and 75 nM in cell-based assays). Originally reported to exhibit >200-fold selectivity for the D₂ receptor versus other dopamine receptor subtypes (K_i values are 9.0, 1940, >2190 and >7140 for D₂, D₃, D₄ and D₁ receptors respectively). More recently reported to be around 32-fold selective for D₂ over D₃ receptors (K_i values are 17.1 and 546 nM respectively). Exhibits antiParkinsonian activity.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt	319.31
Formula	C₁₁H₁₃N₃O.C₄H₄O₄
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	179386-44-8
PubChem ID	9818478
InChI Key	VOJRMYBBPKNLLI-ORHWHDKWSA-N
Smiles	O=C3N2C1=C(N3)C=CC=C1C[C@@H](NC)C2.O=C(/C=CC(O)=O)O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	31.93	100
	water	31.93	100

Preparing Stock Solutions

The following data is based on the product molecular weight 319.31. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.13 mL	15.66 mL	31.32 mL
5 mM	0.63 mL	3.13 mL	6.26 mL
10 mM	0.31 mL	1.57 mL	3.13 mL
50 mM	0.06 mL	0.31 mL	0.63 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

McCall et al (2005) Sumanirole, a highly dopamine D₂-selective receptor agonist: in vitro and in vivo pharmacological characterization and efficacy in animal models of Parkinson's disease. J.Pharmacol.Exp.Ther. 314 1248 PMID: 15980060

Stephenson et al (2005) The effects of a selective dopamine D₂ receptor agonist on behavioral and pathological outcome in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-treated squirrel monkeys. J.Pharmacol.Exp.Ther. 314 1257 PMID: 15980058

Zou et al (2016) Novel analogues of (R)-5-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) provide clues to Dopamine D₂/D₃ receptor agonist selectivity. J.Med.Chem. 59 2973 PMID: 27035329

Keywords: Sumanirole maleate, supplier, pfizer, dopamine, dopaminergic, receptors, d2, selective, antiparkinsonian, parkinsons, parkinson's, D2, Receptors, D2, Receptors, Tocris Bioscience

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