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Mardepodect (PF-2545920)

Name: Mardepodect (PF-2545920)
Brand: Selleck Chemicals
SKU: S2687
Rating: 5 (7 reviews)

Catalog No.S2687

For research use only.

Mardepodect (PF-2545920) is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE.

Mardepodect (PF-2545920) Chemical Structure

CAS No. 1292799-56-4

Selleck's Mardepodect (PF-2545920) has been cited by 7 Publications

4 Customer Reviews

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PDE Signaling Pathway Map

Biological Activity

Description

Mardepodect (PF-2545920) is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE.

Targets

PDE10A ^[2]
(Cell-free assay)

0.37 nM

In vitro

PF-2545920 shows excellent potency and selectivity of PDE10A with IC50 of 1.26 nM. ^[1]

In vivo

PF-2545920 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]

Protocol (from reference)

Animal Research: ^[2]	Animal Models: Jugular vein-cannulated male Sprague-Dawley rats Dosages: 0.1 mg/kg Administration: Inject intravenous through jugular vein catheter in a single dose 4 hours before feed

References

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	392.45
Formula	C₂₅H₂₀N₄O
CAS No.	1292799-56-4
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CN1C=C(C(=N1)C2=CC=C(C=C2)OCC3=NC4=CC=CC=C4C=C3)C5=CC=NC=C5

Download Mardepodect (PF-2545920) SDF

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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