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Chemical Structure : SB269652
Catalog No.: PC-42975Not For Human Use, Lab Use Only.
SB269652 is a potent, selective, negative allosteric modulator of dopamine D2 and D3 receptors, abolishes specific binding of [3H]nemanopride and [3H]spiperone to CHO-transfected D3 receptors with IC50 of1.86 and 0.18 nM.
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SB269652 is a potent, selective, negative allosteric modulator of dopamine D2 and D3 receptors, abolishes specific binding of [3H]nemanopride and [3H]spiperone to CHO-transfected D3 receptors with IC50 of1.86 and 0.18 nM.
SB269652 potently blocks D3 receptor-mediated activation of Gα(i3) and phosphorylation of ERK1/2 at 1-10 uM, partially (35%) inhibits the dopamine-induced recruitment of β-arrestin2 to D2 receptors.
SB269652 is actually a negative allosteric modulator of D2- and D3-receptor dimers.
| M.Wt | 426.5533 | |
| Formula | C27H30N4O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Shonberg J, et al. J Med Chem. 2015 Jul 9;58(13):5287-307.
2. Lane JR, et al. Nat Chem Biol. 2014 Sep;10(9):745-52.
3. Silvano E, et al. Mol Pharmacol. 2010 Nov;78(5):925-34.
4. Rossi M, et al. Mol Pharmacol. 2017 Jun;91(6):586-594.
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