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PF-592379

Catalog No. T10080 CAS 710655-15-5

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

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PF-592379, CAS 710655-15-5

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Attkins N, et al. Pharmacokinetics and elucidation of the rates and routes of N-glucuronidation of PF-592379, an oral dopamine 3 agonist in rat, dog, and human. Xenobiotica. 2010 Nov;40(11):730-42. 2. Wager TT, et al. Dopamine D3/D2 Receptor Antagonist PF-4363467 Attenuates Opioid Drug-Seeking Behavior without Concomitant D2 Side Effects. ACS Chem Neurosci. 2017 Jan 18;8(1):165-177. 3. Collins GT, et al. Lack of abuse potential in a highly selective dopamine D3 agonist, PF-592,379, in drug self-administration and drug discrimination in rats. Behav Pharmacol. 2012 Jun;23(3):280-91.

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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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.

Keywords

PF-592379 710655-15-5 Others PF 592379 PF592379 inhibitor inhibit

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