Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PF-592379 is a potent agonist of dopamine D3 receptor (EC50: 21 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,520.00 | |
50 mg | 6-8 weeks | $ 1,980.00 | |
100 mg | 6-8 weeks | $ 2,500.00 |
Description | PF-592379 is a potent agonist of dopamine D3 receptor (EC50: 21 nM). |
Targets&IC50 | D3 receptor:(EC50)21 nM |
In vitro | PF-592379 appears to be a full agonist (Emax=95%) when compared with the standard Pramipexole [1]. PF-592379 is a potent and selective dopamine 3 agonist (EC50: 21 nM; Ki: 322 nM) [2]. PF-592379 selectively binds human D3 receptors with a high affinity (Ki: 215 nM). Although PF-592379 also binds to human D4 receptors (Ki: 4165 nM), it displays a 19-fold binding selectivity for human D3 over D4 receptors. PF-592379 fails to bind D1 (Ki≥10 μM), human D2 (Ki≥10 μM), or D5 (Ki≥10 μM) receptors at concentrations of up to 10 μM [3]. |
In vivo | PF-592379 acts as an oral dopamine 3 agonist in rats and dogs. It exhibits a clearance rate of 6.3 and 8.5 mL/min/kg in dogs and 44.8 and 58.2 mL/min/kg in rats, considered low to moderate relative to liver blood flow. The compound demonstrates high permeability in Caco-2 cells and shows complete absorption in pharmacokinetic studies carried out on rats and dogs, achieving oral bioavailability rates of 28% in rats and 61 to 87% in dogs [1]. |
Molecular Weight | 235.33 |
Formula | C13H21N3O |
CAS No. | 710655-15-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
PF-592379 710655-15-5 Others PF 592379 PF592379 inhibitor inhibit