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PF-05180999 (PF-999) is a selective and potent phosphodiesterase 2A (PDE2A) inhibitor that enhances long-term memory in a contextual fear conditioned reflex model in rats.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $40 | - | In Stock | |
| 5 mg | $64 | - | In Stock | |
| 10 mg | $113 | - | In Stock | |
| 25 mg | $239 | - | In Stock | |
| 50 mg | $396 | - | In Stock | |
| 100 mg | $691 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $71 | - | In Stock |
| Description | PF-05180999 (PF-999) is a selective and potent phosphodiesterase 2A (PDE2A) inhibitor that enhances long-term memory in a contextual fear conditioned reflex model in rats. |
| Targets&IC50 | PDE11A4:50.09 μM, PDE2A (dog):8.4 nM (Ki), PDE10A1:2.03 μM, PDE2A (monkey):3.4 nM, PDE7B:26.969 μM, PDE2A (dog):5.2 nM, PDE2A (monkey):5.5 nM (Ki), PDE2A (rat):2.6 nM, PDE2A (rat):4.2 nM (Ki) |
| In vitro | PF-05180999 is a weak inducer of CYP3A4 with no direct inhibition of human recombinant cytochrome P450 enzymes (including 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A) and does not induce CYP1A2.PF-05180999 binds to PDE2A in rat, dog, and monkey with Ki values of 4.2 nM 8.4 nM, and 5.5 nM, with IC50 values of 2.6 nM, 5.2 nM, and 3.4 nM, respectively.For the other PDE isoforms, PF-05180999 was weakly active, 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). [1] |
| In vivo | PF-05180999 induced an acute, dose-dependent increase in cGMP levels in mouse cortex, striatum and hippocampus, but had no effect on cAMP levels and its downstream phosphorylated cAMP response element binding protein (p-CREB). In the radial arm maze (RAM) model of working memory, subcutaneous injection of 0.032-0.32 mg/kg PF-05180999 significantly reduced ketamine-induced working memory errors in rats. [1] |
| Synonyms | PF-999, PF999, PF-5180999, PF5180999, PF05180999 |
| Molecular Weight | 414.39 |
| Formula | C19H17F3N8 |
| Cas No. | 1394033-54-5 |
| Smiles | FC(F)(F)C=1C=NC(=CC1)C2=C(C=NN2C)C=3N=C(N4N=CN=C(C34)N5CCC5)C |
| Relative Density. | 1.57 g/cm3 (Predicted) |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 40 mg/mL (96.53 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.83 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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