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CCG-63802

Chemical Structure : CCG-63802

CAS No.: 620112-78-9

CCG-63802 (CCG 63802;CCG63802)

Catalog No.: PC-45955Not For Human Use, Lab Use Only.

A reversible, allosteric inhibitor of regulator of G-protein signaling (RGS) proteins with a potency order of RGS4 > 19 = 16 > 8 >> 7.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

A reversible, allosteric inhibitor of regulator of G-protein signaling (RGS) proteins with a potency order of RGS4 > 19 = 16 > 8 >> 7; inhibits the Gαo-RGS4 interaction with IC50 of 1.9 uM, does not inhibit Gα binding to RGS7, 2- to 10-fold more potent at RGS4 than on the other closely related R4 family members, RGS8 and RGS16; decreases neuropathic hyperalgesia and restores cannabinoid CB1 receptor signalling in PSNL rats.

Physicochemical Properties

M.Wt 450.5117
Formula C26H18N4O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Benzothiazoleacetonitrile, .alpha.-[[9-methyl-2-(3-methylphenoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-3-yl]methylene]-

References

1. Blazer LL, et al. Mol Pharmacol. 2010 Sep;78(3):524-33.

2. Bosier B, et al. Br J Pharmacol. 2015 Nov;172(22):5333-46.

3. Dobrivojević M, et al. Am J Physiol Cell Physiol. 2012 Dec 15;303(12):C1260-8.

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