PF-2545920

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PF-2545920 is available in the following compound libraries:

Chemical Library (96-well) Inhibitor Library (96-well) Pfizer Licensed Library

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PF-2545920 Mechanism
PF-2545920 Mechanism
Phosphodiesterase(PDE) comprises three types of subunits: the two heavy conserved C-terminal catalytic domains, PDE alpha and PDE beta and the N-terminal regulatory region, PDE gamma. ^[1] The catalytic domains of Phosphodiesterases share a common function and have a much more conserved structure. The PDE active site forms a deep pocket lined with highly conserved residues, while Zn2+ binding site and Mg2+ binding site are located at the wider side of the active site. ^[2]
The crystal structure indicates that PF-2545920 binds in the active site of PDE 10A. Specifically, the quinoline moiety of PF-2545920 deeply extends into a selectivity pocket and forms a hydrogen bond to the side chain of Tyr683. Besides the carbonyl group also makes an H-bond to the side chain of Tyr683. The pyrazole ring extends towards the metal ion binding site and is involved in the interactions mediated by water molecules. Furthermore, the pyridine ring makes a water-bridging hydrogen bond interaction to Thr675. The interactions contributes to the high potency and selectivity of PF-2545920 against PDE 10A. ^[3]
References [1] Deterre P, et al. Proc Natl Acad Sci. U.S.A. 1988, 85(8), 2424-2428.
[2] Card GL, et al. Structure. 2004, 12(12), 2233-2247.
[3] Verhoest PR, et al. J Med Chem. 2009, 52(16), 5188-5196.
Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Cat.No.	Product Name	Solubility (25°C)
S1512	Tadalafil (Cialis)	<1 mg/mL	78 mg/mL	<1 mg/mL
S1431	Sildenafil citrate	<1 mg/mL	23 mg/mL	<1 mg/mL
S2620	GSK256066	<1 mg/mL	5 mg/mL	<1 mg/mL
S1430	Rolipram	<1 mg/mL	55 mg/mL	55 mg/mL
S1455	Cilomilast (SB-207499)	<1 mg/mL	69 mg/mL	50 mg/mL
S2131	Roflumilast (Daxas)	<1 mg/mL	81 mg/mL	18 mg/mL
S2515	Vardenafil Hydrochloride Trihydrate (Vivanza)	116 mg/mL	116 mg/mL	20 mg/mL
S2687	PF-2545920	<1 mg/mL	79 mg/mL	79 mg/mL
S1294	Cilostazol	<1 mg/mL	74 mg/mL	6 mg/mL
S1550	Pimobendan (Vetmedin)	<1 mg/mL	67 mg/mL	5 mg/mL
S1504	Dyphylline (Dilor)	51 mg/mL	51 mg/mL	<1 mg/mL
S1673	Aminophylline (Truphylline)	84 mg/mL	53 mg/mL	<1 mg/mL
S2127	S-(+)-Rolipram	<1 mg/mL	55 mg/mL	55 mg/mL
S3172	Anagrelide HCl	<1 mg/mL	14 mg/mL	<1 mg/mL
S4019	Avanafil	<1 mg/mL	97 mg/mL	<1 mg/mL
S8034	Apremilast (CC-10004)	<1 mg/mL	92 mg/mL	<1 mg/mL

Product Description

Biological Activity Protocol Chemical Information Tech Support & FAQs

Biological Activity

Description	PF-2545920 is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM.
Targets	PDE10A
IC50	0.37 nM ^[2]
In vitro	MP-10 shows excellent potency and selectivity of PDE10A with IC50 of 1.26 nM. ^[1]
In vivo	MP-10 intraperitoneally administrated at dose of 0.3, 3, and 5 mg/kg in male CF-1 mice causes striking increases in GluR1 phosphorylation levels of 3-, 5.4-, and 4.1-fold , respectively. MP-10 at concentration of 1 μM treats Rat striatal slices for 30 min, the level of GluR1S845 phosphorylation at the cell surface is significantly increased 2-fold, without change the level of total GluR1 on the cell surface. MP-10 intraperitoneally administrated at dose of 0.3, 3, and 5 mg/kg in male CF-1 mice results in robust, statistically significant increases in CREBS133 phosphorylation of 3-, 4-, and 2.6-fold, respectively. MP-10 intraperitoneally administrated at dose of 3 mg/kg increases both enkephalin and substance-P mRNA levels in striatum of CF-1 mice. MP-10 intraperitoneally administrated at dose of 0.3-1 mg/kg decreases avoidance responding with a significant treatment effect in the mouse CAR model. Mice treated with MP-10 at dose of 0.03 mg/kg spents more time in the empty than social side in the mice, MP-10 also dose-dependently decreased locomotor activity. ^[1] PDE10A subcutaneously administrated at dose of 1 mg/kg elevates striatal cGMP about 3 fold in male CD-1 mice, while PDE10A subcutaneously administrated at dose of 3.2 mg/kg displays a maximal elevation of striatal cGMP approximately a 5-fold increase in male CD-1 mice. PDE10A intravenous injected at a dose of 0.1 mg/kg in Sprague-Dawley rats displays clearance of 36 ml/min/Kg, DE10A intravenous injected at a dose of 0.3 mg/kg in Dog Beagle displays clearance of 7.2 ml/min/Kg in vivo clearance with a moderate volume of distribution, DE10A intravenous injected at a dose of 0.03 mg/kg in Monkey Cynomolgus displays clearance of 13.9 ml/min/Kg in vivo clearance with a moderate volume of distribution. PDE10A is active with an ED50 of 1 mg/kg at a significantly lower total plasma exposure (115 nM) in the conditioned avoidance response assay (CAR) in Sprague-Dawley rats. ^[2]
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Protocol(Only for Reference)

1

References

Chemical Information

Download PF-2545920 SDF

Molecular Weight (MW)	392.45
Formula	C₂₅H₂₀N₄O
CAS No.	1292799-56-4
Synonyms	N/A

Solubility (25°C) DMSO 79 mg/mL Water <1 mg/mL Ethanol 79 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name	2-((4-(1-methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl)phenoxy)methyl)quinoline

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Validation & Quality Control

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Related Compound Libraries

PF-2545920 is available in the following compound libraries:

Product Information

Compare PDE Inhibitors

PF-2545920 Mechanism

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Biological Activity

Protocol(Only for Reference)

References

Chemical Information

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Related PDE Inhibitors

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Cat.No.	Product Name	Solubility (25°C)
Cat.No.	Product Name	Water	DMSO	Ethanol
S1512	Tadalafil (Cialis)	<1 mg/mL	78 mg/mL	<1 mg/mL
S1431	Sildenafil citrate	<1 mg/mL	23 mg/mL	<1 mg/mL
S2620	GSK256066	<1 mg/mL	5 mg/mL	<1 mg/mL
S1430	Rolipram	<1 mg/mL	55 mg/mL	55 mg/mL
S1455	Cilomilast (SB-207499)	<1 mg/mL	69 mg/mL	50 mg/mL
S2131	Roflumilast (Daxas)	<1 mg/mL	81 mg/mL	18 mg/mL
S2515	Vardenafil Hydrochloride Trihydrate (Vivanza)	116 mg/mL	116 mg/mL	20 mg/mL
S2687	PF-2545920	<1 mg/mL	79 mg/mL	79 mg/mL
S1294	Cilostazol	<1 mg/mL	74 mg/mL	6 mg/mL
S1550	Pimobendan (Vetmedin)	<1 mg/mL	67 mg/mL	5 mg/mL
S1504	Dyphylline (Dilor)	51 mg/mL	51 mg/mL	<1 mg/mL
S1673	Aminophylline (Truphylline)	84 mg/mL	53 mg/mL	<1 mg/mL
S2127	S-(+)-Rolipram	<1 mg/mL	55 mg/mL	55 mg/mL
S3172	Anagrelide HCl	<1 mg/mL	14 mg/mL	<1 mg/mL
S4019	Avanafil	<1 mg/mL	97 mg/mL	<1 mg/mL
S8034	Apremilast (CC-10004)	<1 mg/mL	92 mg/mL	<1 mg/mL

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PF-2545920

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

PF-2545920 is available in the following compound libraries:

Product Information

Compare PDE Inhibitors

PF-2545920 Mechanism

Product Description

Biological Activity

Protocol(Only for Reference)

References

Chemical Information

Research Area

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If you have any other enquiries, please leave a message.

Related PDE Inhibitors

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