PF-592379

Name: PF-592379
Brand: TargetMol
SKU: T10080
Rating: 4.5 (1 reviews)

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产品编号 T10080Cas号 710655-15-5

PF-592379 is a potent agonist of dopamine D3 receptor (EC50: 21 nM).

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产品编号 T10080Cas号 710655-15-5

PF-592379 is a potent agonist of dopamine D3 receptor (EC50: 21 nM).

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产品描述	PF-592379 is a potent agonist of dopamine D3 receptor (EC50: 21 nM).
靶点活性	D3 receptor:（EC50）21 nM
体外活性	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].
体内活性	In rats and dogs, PF-592379 is an oral dopamine 3 agonist. PF-592379 has low-moderate clearance relative to liver blood flow of 6.3 and 8.5 mL/min/kg in dog and 44.8 and 58.2 mL/min/kg in rats. It has high permeability in Caco-2 cells and is completely absorbed in rat and dog pharmacokinetic studies with an oral bioavailability of 28% in both rats and 61 and 87% in the dogs [1].