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    InvivoChem Cat #: V4449
    CAS #: 710655-15-5Purity ≥98%

    Description: PF-592379 is a novel, potent and selective agonist of dopamine D3 receptor agonist with an EC50 of 21 nM. PF-592379 has the potential for the treatment of male erectile dysfunction and female sexual dysfunction. opamine receptor antagonism is a compelling molecular target for the treatment of a range of psychiatric disorders, including substance use disorders. In vivo, 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 rat. It has high permeability in Caco-2 cells and was completely absorbed in rat and dog pharmacokinetic studies with an oral bioavailability of 28% in both rats and 61 and 87% in the dogs. These data are consistent with the physicochemical properties of PF-592379, which indicate complete absorption by the transcellular route. Elimination of PF-592379 was predominantly metabolic in nature. In vitro routes of metabolism studies indicate that metabolism in the rat is a combination of P450 mechanisms and N-glucuronidation, whereas in dog and human, N-glucuronidation is the major route. NMR analysis indicates that N-glucuronidation is non-quaternary in nature and occurs on both the pyridyl amine and ring nitrogen. Rates of clearance via N-glucuronidation were predicted to be low in humans compared with acyl or phenolic glucuronidation. PF-592379 was predicted to have complete absorption from the gastrointestinal tract and an oral bioavailability of >60% in the clinic. Clinical data verified that PF-592379 is a low clearance compound in human, with a mean oral clearance of 6.5 ml/min/kg following a 200 mg oral dose. PF-592379 has ideal pharmacokinetic properties for an oral D3 agonist, intended for on demand dosing.

    References:  2017 Jan 18;8(1):165-177;  2010 Nov;40(11):730-42; 

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    Name: PF-592379
    CAS#: 710655-15-5
    Chemical Formula: C13H21N3O
    Exact Mass: 235.1685
    Molecular Weight: 235.33
    Elemental Analysis: C, 66.35; H, 8.99; N, 17.86; O, 6.80
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: PF-592379; PF 592379; PF592379.
    IUPAC/Chemical Name: 5-[(2R,5S)-5-methyl-4-propylmorpholin-2-yl]pyridin-2-amine
    InChi Code: InChI=1S/C13H21N3O/c1-3-6-16-8-12(17-9-10(16)2)11-4-5-13(14)15-7-11/h4-5,7,10,12H,3,6,8-9H2,1-2H3,(H2,14,15)/t10-,12-/m0/s1
    SMILES Code: NC1=NC=C([[email protected]@H]2CN(CCC)[[email protected]@H](C)CO2)C=C1

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