[CAS NO. 1454808-95-7] LP-922761
PRODUCTS SPECIFICATIONS [1454808-95-7]
DESCRIPTION [1454808-95-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 410.47 |
| Molecular Formula | C21H26N6O3 |
| SMILES | O=C(N(C)CCNC1=NN2C(C=C1)=NC=C2C3=CC=C(C=C3)C(N)=O)OC(C)(C)C |
Summary
LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1 ) inhibitor with IC 50 s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC 50 of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK) , opioid, adrenergic α2 or GABAa receptors [1] .
IC50 & Target
IC50: 4.8 nM (Adapter protein-2 associated kinase 1 (AAK1) in enzyme assays); 7.6 nM (AAK1 in cell assays); 24 nM (BMP-2-inducible protein kinase (BIKE)) [1]
In Vivo
In mouse, LP-922761 has a brain to plasma ratio of 0.007, indicating that LP-922761 is essentially restricted to the peripheral compartment [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 41.67 mg/mL ( 101.52 mM ; ultrasonic and warming and heat to 80°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4362 mL | 12.1812 mL | 24.3623 mL |
| 5 mM | 0.4872 mL | 2.4362 mL | 4.8725 mL |
| 10 mM | 0.2436 mL | 1.2181 mL | 2.4362 mL |