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PF-05180999
🥰Excellent
Catalog No. T16484Cas No. 1394033-54-5
Alias PF-999, PF999, PF-5180999, PF5180999, PF05180999
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.
PF-05180999
🥰Excellent
Purity: 99.43%
Catalog No. T16484Alias PF-999, PF999, PF-5180999, PF5180999, PF05180999Cas No. 1394033-54-5
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 | Availability | Quantity |
|---|---|---|---|
| 2 mg | $82 | In Stock |
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CitedSelect Batch
Purity:99.43%
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Product Introduction
Bioactivity
Chemical Properties
| 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 | PDE7B:26.969 μM, PDE2A (monkey):3.4 nM, PDE2A (monkey):5.5 nM (Ki), PDE10A1:2.03 μM, PDE11A4:50.09 μM, PDE2A (rat):4.2 nM (Ki), PDE2A (rat):2.6 nM, PDE2A (dog):5.2 nM, PDE2A (dog):8.4 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] |
| Alias | 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 & Solubility Information
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 40 mg/mL (96.53 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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In Vivo Formulation Calculator (Clear solution)
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:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
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 DMSO (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.
(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 DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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