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CCG258747

$610$4,800

Products Details

Product Description

– CCG258747 is a selective GRK2 inhibitor (IC50=18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, >5500, and >550–fold, respectively).CCG258747 also blocks the internalization of the µ-opioid receptor. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure[1].

Web ID

– HY-139690

Storage Temperature

– 4°C (Powder, sealed storage, away from moisture and light)

Shipping

– Room Temperature

Molecular Formula

– C28H27FN4O4

References

– [1]Renee A Bouley, et al. A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of the μ-Opioid Receptor. Mol Pharmacol. 2020 Jun;97(6):392-401.

CAS Number

– 2615910-00-2

Molecular Weight

– 502.54

Compound Purity

– 99.17

SMILES

– O=C(NCC1=NNC2=CC=CC=C12)C(C=C3[C@@](CCNC4)([H])[C@@H]4COC5=CC=C(OCO6)C6=C5)=C(C=C3)F

Clinical Information

– No Development Reported

Research Area

– Cardiovascular Disease

Solubility

– DMSO : 100 mg/mL (ultrasonic)

Target

– Opioid Receptor

Pathway

– GPCR/G Protein;Neuronal Signaling

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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