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SB269652

Catalog No. T16857 CAS 215802-15-6

SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor.

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SB269652, CAS 215802-15-6

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,430.00
50 mg	6-8 weeks	$ 1,860.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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Description

SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor.

In vitro

D3 receptor antagonist SB269,652 effectively abolished specific binding of [(3)H]nemanopride and [(3)H]spiperone to Chinese hamster ovary-transfected D(3) receptors when radioligands were used at 0.2 and 0.5 nM, respectively. However, SB269,652 only submaximally inhibited the specific binding of these radioligands when they were employed at 10-fold higher concentrations even at high concentrations (5 μM). By analogy, although SB269,652 potently blocked D(3) receptor-mediated activation of Gα(i3) and phosphorylation of extracellular-signal-regulated kinase (ERK)1/2, when concentrations of dopamine were increased by 10-fold, from 1 μM to 10 μM, SB269,652 only submaximally inhibited dopamine-induced stimulation of Gα(i3) [1].

Molecular Weight	426.55
Formula	C27H30N4O
CAS No.	215802-15-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Silvano E, et al. The tetrahydroisoquinoline derivative SB269,652 is an allosteric antagonist at dopamine D3 and D2 receptors. Mol Pharmacol. 2010 Nov;78(5):925-34. 2. Lane JR, et al. A new mechanism of allostery in a G protein-coupled receptor dimer. Nat Chem Biol. 2014 Sep;10(9):745-52. 3. Presgraves SP, et al. Involvement of dopamine D(2)/D(3) receptors and BDNF in the neuroprotective effects of S32504 and pramipexole against 1-methyl-4-phenylpyridinium in terminally differentiated SH-SY5Y cells. Exp Neurol. 2004 Nov;190(1):157-70.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SB269652 215802-15-6 Others SB-269652 SB 269652 inhibitor inhibit

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