PF 5006739

Names

[ Name ]:
PF 5006739

[Synonym ]:
4-{4-(4-Fluorophenyl)-1-[1-(1,2-Oxazol-3-Ylmethyl)piperidin-4-Yl]-1h-Imidazol-5-Yl}pyrimidin-2-Amine
2-Pyrimidinamine, 4-[4-(4-fluorophenyl)-1-[1-(3-isoxazolylmethyl)-4-piperidinyl]-1H-imidazol-5-yl]-
4-{4-(4-Fluorophenyl)-1-[1-(1,2-oxazol-3-ylmethyl)-4-piperidinyl]-1H-imidazol-5-yl}-2-pyrimidinamine

Biological Activity

[Description]:

PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid drug-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner[1]. PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity[2].

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> Casein Kinase

Research Areas >> Neurological Disease

Signaling Pathways >> Stem Cell/Wnt >> Casein Kinase

[Target]

CK1δ:3.9 nM (IC50)

CK1ϵ:17.0 nM (IC50)

[References]

[1]. Wager TT, et al. Casein kinase 1δ/ε inhibitor PF-5006739 attenuates opioid drug-seeking behavior. ACS Chem Neurosci. 2014 Dec 17;5(12):1253-65.

[2]. Cunningham PS, et al. Targeting of the circadian clock via CK1δ/ε to improve glucose homeostasis in obesity.Sci Rep. 2016 Jul 21;6:29983.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
680.9±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₂H₂₂FN₇O

[ Molecular Weight ]:
419.455

[ Flash Point ]:
365.6±34.3 °C

[ Exact Mass ]:
419.186981

[ LogP ]:
2.26

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.718

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310

[ Hazard Codes ]:
T+

[ RIDADR ]:
UN 2811 6.1 / PGIII

Related Compounds

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