CCG258747

Chemical Structure : CCG258747

CAS No.: 2615910-00-2

Catalog No.: PC-23973Not For Human Use, Lab Use Only.

CCG258747 is a potent selective GRK2 inhibitor with IC50 of 18 nM, 83-fold selectivity over GRK5.

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2 mg	$258	In stock
5 mg	$458	In stock
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Biological Activity

CCG258747 is a potent selective GRK2 inhibitor with IC50 of 18 nM, 83-fold selectivity over GRK5.
CCG258747 is selective against GRK1 and PKA and shows little inhibition against ROCK1 at 10 µM.
CCG258747 demonstrated robust efficacy in blocking receptor internalization in HEK293 cells.
CCG258747 reduced MOR phosphorylation of Ser375 in pSer375-MOR for both HEK293 and U2OS stable cells.

Physicochemical Properties

M.Wt	502.55
Formula	C28H27FN4O4
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	Benzamide, 5-[(3S,4R)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-piperidinyl]-2-fluoro-N-(1H-indazol-3-ylmethyl)-

References

1. Bouley RA, et al. Mol Pharmacol. 2020 Jun;97(6):392-401.

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CCG258747

Biological Activity

Physicochemical Properties

References

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