PF 4800567 hydrochloride

CAS# 1391052-28-0

PF 4800567 hydrochloride

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Chemical structure

PF 4800567 hydrochloride

3D structure

Chemical Properties of PF 4800567 hydrochloride

Cas No. 1391052-28-0 SDF Download SDF
PubChem ID 71751553 Appearance Powder
Formula C17H19Cl2N5O2 M.Wt 396.27
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO
Chemical Name 3-[(3-chlorophenoxy)methyl]-1-(oxan-4-yl)pyrazolo[3,4-d]pyrimidin-4-amine;hydrochloride
SMILES C1COCCC1N2C3=C(C(=N2)COC4=CC(=CC=C4)Cl)C(=NC=N3)N.Cl
Standard InChIKey QZXZQMUZEHTFHD-UHFFFAOYSA-N
Standard InChI InChI=1S/C17H18ClN5O2.ClH/c18-11-2-1-3-13(8-11)25-9-14-15-16(19)20-10-21-17(15)23(22-14)12-4-6-24-7-5-12;/h1-3,8,10,12H,4-7,9H2,(H2,19,20,21);1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of PF 4800567 hydrochloride

DescriptionSelective casein kinase 1ε inhibitor; displays 22-fold greater potency towards CK1ε than CK1δ (IC50 values are 32 and 711 nM for CK1ε and CK1δ respectively). ATP competitive. Displays minimal effect on the circadian clock.

PF 4800567 hydrochloride Dilution Calculator

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PF 4800567 hydrochloride Molarity Calculator

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Preparing Stock Solutions of PF 4800567 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5235 mL 12.6177 mL 25.2353 mL 50.4706 mL 63.0883 mL
5 mM 0.5047 mL 2.5235 mL 5.0471 mL 10.0941 mL 12.6177 mL
10 mM 0.2524 mL 1.2618 mL 2.5235 mL 5.0471 mL 6.3088 mL
50 mM 0.0505 mL 0.2524 mL 0.5047 mL 1.0094 mL 1.2618 mL
100 mM 0.0252 mL 0.1262 mL 0.2524 mL 0.5047 mL 0.6309 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on PF 4800567 hydrochloride

Pharmacological studies of 3-[bis(3,3-diphenylpropyl)-amino]-propan-1-ol hydrochloride, (PF-244), a new cerebral vasodilator.[Pubmed:1174078]

Arzneimittelforschung. 1975 Apr;25(4):632-8.

Pharmacological effects of 3-[bis(3,3-diphenylpropyl)-amino]-propan-1-ol-hydrochloride (PF-244) mainly on cerebral and cardiovascular systems, were studied. PF-244 indicated a potent cerebral vasodilation effect and a marked increase in oxygen supply to cerebral tissue with only weak inotropic action and depressor effect. This cerebral vasodilation was more potent and specific than that of papaverine hydrochloride in regional cerebral flow. PF-244 also indicated an antibarium action, although it did not show the properties related to the cholinergic and/or adrenergic mechanism. PF-244 appears to be one of the potent cerebral vascular dilators, and the nature of its mechanism was discussed.

Casein kinase 1 delta (CK1delta) regulates period length of the mouse suprachiasmatic circadian clock in vitro.[Pubmed:20421981]

PLoS One. 2010 Apr 22;5(4):e10303.

BACKGROUND: Casein kinase 1 delta (CK1delta) plays a more prominent role in the regulation of circadian cycle length than its homologue casein kinase 1 epsilon (CK1epsilon) in peripheral tissues such as liver and embryonic fibroblasts. Mice lacking CK1delta die shortly after birth, so it has not been possible to assess the impact of loss of CK1delta on behavioral rhythms controlled by the master circadian oscillator in the suprachiasmatic nuclei (SCN). METHODOLOGY/PRINCIPAL FINDINGS: In the present study, mPER2::LUCIFERASE bioluminescence rhythms were monitored from SCN explants collected from neonatal mice. The data demonstrate that SCN explants from neonatal CK1delta-deficient mice oscillate, but with a longer circadian period than littermate controls. The cycle length of rhythms recorded from neonatal SCN explants of CK1epsilon-deficient mice did not differ from control explants. CONCLUSIONS/SIGNIFICANCE: The results indicate that CK1delta plays a more prominent role than CK1epsilon in the maintenance of 24-hour rhythms in the master circadian oscillator.

Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes.[Pubmed:20696890]

Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15240-5.

Circadian pacemaking requires the orderly synthesis, posttranslational modification, and degradation of clock proteins. In mammals, mutations in casein kinase 1 (CK1) epsilon or delta can alter the circadian period, but the particular functions of the WT isoforms within the pacemaker remain unclear. We selectively targeted WT CK1epsilon and CK1delta using pharmacological inhibitors (PF-4800567 and PF-670462, respectively) alongside genetic knockout and knockdown to reveal that CK1 activity is essential to molecular pacemaking. Moreover, CK1delta is the principal regulator of the clock period: pharmacological inhibition of CK1delta, but not CK1epsilon, significantly lengthened circadian rhythms in locomotor activity in vivo and molecular oscillations in the suprachiasmatic nucleus (SCN) and peripheral tissue slices in vitro. Period lengthening mediated by CK1delta inhibition was accompanied by nuclear retention of PER2 protein both in vitro and in vivo. Furthermore, phase mapping of the molecular clockwork in vitro showed that PF-670462 treatment lengthened the period in a phase-specific manner, selectively extending the duration of PER2-mediated transcriptional feedback. These findings suggested that CK1delta inhibition might be effective in increasing the amplitude and synchronization of disrupted circadian oscillators. This was tested using arrhythmic SCN slices derived from Vipr2(-/-) mice, in which PF-670462 treatment transiently restored robust circadian rhythms of PER2::Luc bioluminescence. Moreover, in mice rendered behaviorally arrhythmic by the Vipr2(-/-) mutation or by constant light, daily treatment with PF-670462 elicited robust 24-h activity cycles that persisted throughout treatment. Accordingly, selective pharmacological targeting of the endogenous circadian regulator CK1delta offers an avenue for therapeutic modulation of perturbed circadian behavior.

Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period.[Pubmed:19458106]

J Pharmacol Exp Ther. 2009 Aug;330(2):430-9.

The circadian clock links our daily cycles of sleep and activity to the external environment. Deregulation of the clock is implicated in a number of human disorders, including depression, seasonal affective disorder, and metabolic disorders. Casein kinase 1 epsilon (CK1epsilon) and casein kinase 1 delta (CK1delta) are closely related Ser-Thr protein kinases that serve as key clock regulators as demonstrated by mammalian mutations in each that dramatically alter the circadian period. Therefore, inhibitors of CK1delta/epsilon may have utility in treating circadian disorders. Although we previously demonstrated that a pan-CK1delta/epsilon inhibitor, 4-[3-cyclohexyl-5-(4-fluoro-phenyl)-3H-imidazol-4-yl]-pyrimidin-2-ylamine (PF-670462), causes a significant phase delay in animal models of circadian rhythm, it remains unclear whether one of the kinases has a predominant role in regulating the circadian clock. To test this, we have characterized 3-(3-chloro-phenoxymethyl)-1-(tetrahydro-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin- 4-ylamine (PF-4800567), a novel and potent inhibitor of CK1epsilon (IC(50) = 32 nM) with greater than 20-fold selectivity over CK1delta. PF-4800567 completely blocks CK1epsilon-mediated PER3 nuclear localization and PER2 degradation. In cycling Rat1 fibroblasts and a mouse model of circadian rhythm, however, PF-4800567 has only a minimal effect on the circadian clock at concentrations substantially over its CK1epsilon IC(50). This is in contrast to the pan-CK1delta/epsilon inhibitor PF-670462 that robustly alters the circadian clock under similar conditions. These data indicate that CK1epsilon is not the predominant mediator of circadian timing relative to CK1delta. PF-4800567 should prove useful in probing unique roles between these two kinases in multiple signaling pathways.

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