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CCG215022

Cat. No. M8923
CCG215022 Structure
Size Price Availability
5mg USD 440 4-7 Days
10mg USD 625 4-7 Days
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50 values of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, GRK5 and GRK1, respectively. In the course of a GRK2 structure-based drug design campaign, CCG215022 exhibits nanomolar IC50 values against both GRK2 and GRK5 and good selectivity against other closely related kinases such as GRK1 and PKA. Treatment of murine cardiomyocytes with CCG215022 results in significantly increases contractility at 20-fold lower concentrations than Paroxetine, an inhibitor with more modest selectivity for GRK2.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 499.5
Formula C26H22FN7O3
CAS Number 1813527-81-9
Purity >98%
Solubility DMSO: ≥ 10 mg/mL
Storage at -20°C
References

Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor.
Homan KT, et al. J Biol Chem. 2015 Aug 21;290(34):20649-59. PMID: 26032411.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CCG215022 supplier, PKA, inhibitors

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