CCG258208 hydrochloride
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 488.94 |
| Molecular Formula | C24H26ClFN4O4 |
| SMILES | FC1=C(C(NCC2=NNC=C2)=O)C=C([C@H]3[C@H](COC4=CC=C(OCO5)C5=C4)CNCC3)C=C1.[H]Cl |
Summary
CCG258208 (GRK2-IN-1) hydrochloride is a potent and selective GRK2 ( G protein-coupled receptor kinase 2 ) inhibitor ( IC 50 =30 nM) while maintaining 230-fold selectivity over GRK5 ( IC 50 =7.09 μM) and more than 2500-fold selectivity over GRK1 ( IC 50 =87.3 μM), PKA , and ROCK1 . CCG258208 hydrochloride can be used in heart failure research [1] .
IC50 & Target
|
GRK2 30 nM (IC 50 ) |
GRK5 7.1 μM (IC 50 ) |
In Vitro
CCG258208 (Compound 14as) (0-1 μM; 10 min) shows significant improvement in βAR-stimulated contractility in mouse cardiomyocytes [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | Mouse cardiomyocytes |
| Concentration: | 0, 0.1, 0.5, and 1 μM |
| Incubation Time: | 10 min |
| Result: | Showed a significant increase in contractility at a concentration of only 0.1 µM. |
In Vivo
CCG258208 (Compound 14as) (intraperitoneal injection; 10 mg/kg; once) treatment shows superior half-life in vivo [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | CD-1 mice [1] |
| Dosage: | 10 mg/kg |
| Administration: | Intraperitoneal injection; 10 mg/kg; once |
| Result: | Showed total plasma drug levels after single IP administration that exceed the GRK2 IC 50 for seven hours. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 250 mg/mL ( 511.31 mM ; Need ultrasonic)
H 2 O : 50 mg/mL ( 102.26 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0452 mL | 10.2262 mL | 20.4524 mL |
| 5 mM | 0.4090 mL | 2.0452 mL | 4.0905 mL |
| 10 mM | 0.2045 mL | 1.0226 mL | 2.0452 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (102.26 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.25 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.25 mM); Clear solution