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PF-05180999

PF-05180999
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PF-05180999

Catalog No. T16484Cas No. 1394033-54-5
PF-05180999 is an inhibitor of phosphodiesterase 2A (IC50: 1.6 nM).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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2 mg$825 days
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Product Introduction

Bioactivity
Description
PF-05180999 is an inhibitor of phosphodiesterase 2A (IC50: 1.6 nM).
In vitro
PF-05180999 is also a weak inducer of CYP3A4, and with no direct inhibition of human recombinant cytochrome P450 (CYP) enzymes (1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A) and no induction of CYP1A2. PF-05180999 binds to the rat, dog and monkey PDE2A (Kis: 4.2, 8.4, and 5.5 nM and IC50s: 2.6, 5.2, and 3.4 nM, respectively). PF-05180999 displays weak activity against PDE, with IC50s of 2.03 μM (PDE10A1), 26.969 μM (PDE7B), 50.09 μM (PDE11A4), and >56.25 μM (PDE1B1, PDE3A1, PDE4D3, PDE5A1, PDE6 (bovine), PDE8B, PDE9A1), respectively [1].
In vivo
PF-05180999 triggers an immediate and dose-dependent increase in cGMP levels in the cortex, striatum, and hippocampus without affecting cAMP levels or the downstream phospho-cAMP response element-binding protein (p-CREB) in mice. At doses of 0.032-0.32 mg/kg, administered subcutaneously, it significantly reduces working memory errors caused by ketamine in a rat working memory radial arm maze (RAM) model [1].
Chemical Properties
Molecular Weight414.39
FormulaC19H17F3N8
Cas No.1394033-54-5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 50 mg/mL (120.66 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4132 mL12.0659 mL24.1319 mL120.6593 mL
5 mM0.4826 mL2.4132 mL4.8264 mL24.1319 mL
10 mM0.2413 mL1.2066 mL2.4132 mL12.0659 mL
20 mM0.1207 mL0.6033 mL1.2066 mL6.0330 mL
50 mM0.0483 mL0.2413 mL0.4826 mL2.4132 mL
100 mM0.0241 mL0.1207 mL0.2413 mL1.2066 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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